Download RGUHS (Rajiv Gandhi University of Health Sciences) B.Pharm Important Question Bank (Bachelor of Pharmacy) Medicinal Chemistry I MC I QP Bank (Latest Important Questions Unit Wise)
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
9
5. Blueprint of question paper, for each QP..
Marks distribution
Total
Marks
Sl
No
Chapter
Must Know
Desirable to
Know
Long
Essay
Short
Essay
Short
Answer
I
Basic
Principles of
Medicinal
Chemistry
Physico-
chemical
properties of
drug
molecules
History and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
10 -- 2 12
II
Central
nervous
system
depressants
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR.
10 -- 2+2 14
III
Adrenergic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 2 7
IV
Cholinergic
drugs and
related agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
5 2+2 9
V
Local
anesthetics
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 5
VI
Histamine
and
antihistaminic
agents
Definition,
classification
with
structures
and synthesis
Histamine
structure,
biosynthesis
and biological
activity.
Histamine
- 5 2 7
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
9
5. Blueprint of question paper, for each QP..
Marks distribution
Total
Marks
Sl
No
Chapter
Must Know
Desirable to
Know
Long
Essay
Short
Essay
Short
Answer
I
Basic
Principles of
Medicinal
Chemistry
Physico-
chemical
properties of
drug
molecules
History and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
10 -- 2 12
II
Central
nervous
system
depressants
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR.
10 -- 2+2 14
III
Adrenergic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 2 7
IV
Cholinergic
drugs and
related agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
5 2+2 9
V
Local
anesthetics
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 5
VI
Histamine
and
antihistaminic
agents
Definition,
classification
with
structures
and synthesis
Histamine
structure,
biosynthesis
and biological
activity.
Histamine
- 5 2 7
10
receptors and
its actions
VII
Analgesic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR and
synthesis
.Steroidal
Antiinflammatar
y agents:
Cortisone,
Hydrocortison,
Dexamethasone
Betamethasone
Triamcinolone,
Fluocinolone
-- 5 2+2 9
VIII
Structure and
medicinal uses
of important
prostaglandin
s
Structure
and
medicinal
uses of
important
prostaglandi
ns
-- -- 2 2
IX
Natural
Products
Definition,
classification
with
structures
and synthesis
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
- 5 5
Total 20 30 20 70
* 80 % of the questions shall be from the Must Know area and 20 % shall be from the
Desirable to know area of the Curriculum.
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
9
5. Blueprint of question paper, for each QP..
Marks distribution
Total
Marks
Sl
No
Chapter
Must Know
Desirable to
Know
Long
Essay
Short
Essay
Short
Answer
I
Basic
Principles of
Medicinal
Chemistry
Physico-
chemical
properties of
drug
molecules
History and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
10 -- 2 12
II
Central
nervous
system
depressants
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR.
10 -- 2+2 14
III
Adrenergic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 2 7
IV
Cholinergic
drugs and
related agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
5 2+2 9
V
Local
anesthetics
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 5
VI
Histamine
and
antihistaminic
agents
Definition,
classification
with
structures
and synthesis
Histamine
structure,
biosynthesis
and biological
activity.
Histamine
- 5 2 7
10
receptors and
its actions
VII
Analgesic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR and
synthesis
.Steroidal
Antiinflammatar
y agents:
Cortisone,
Hydrocortison,
Dexamethasone
Betamethasone
Triamcinolone,
Fluocinolone
-- 5 2+2 9
VIII
Structure and
medicinal uses
of important
prostaglandin
s
Structure
and
medicinal
uses of
important
prostaglandi
ns
-- -- 2 2
IX
Natural
Products
Definition,
classification
with
structures
and synthesis
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
- 5 5
Total 20 30 20 70
* 80 % of the questions shall be from the Must Know area and 20 % shall be from the
Desirable to know area of the Curriculum.
11
6. Question paper layout to show which question number will represent which chapter (s)
Long Essay: 2X 10 = 20
1 Basic Principles of medicinal chemistry
2 Central nervous system depressant
Short Essays: 5x 6 = 30
3 Adrenergic drugs
4 Cholinergic drugs and related agents
5 Local anaesthetics
6 Histamine and antihistaminic agents
7 Analgesic agents
8 Natural products
Short Answers: 2X10 = 20
9 Basic Principles of medicinal chemistry
10 Central nervous system depressant
11 Central nervous system depressant
12 Adrenergic drugs
13 Cholinergic drugs and related agents
14 Cholinergic drugs and related agents
15 Histamine and antihistaminic agents
16 Analgesic agents
17 Analgesic agents
18 Structure and medicinal uses of important prostaglandins
7. Scheme of Practical / Clinical Teaching and Assessment:
List the expected practical / clinical competencies.
State the objectives for each competency.
Assign content for the objectives.
Describe the teaching ? learning processes.
Sl No Skills Duration Learning methods
1 Demonstrate the methods of
synthesis of simple organic
compounds used as drugs or
starting materials.
2 Demonstrate the various
methods of filtration,
crystallization, purification.
3 Reason critically and
logically and make
independent judgments
4 Employ scientific
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
9
5. Blueprint of question paper, for each QP..
Marks distribution
Total
Marks
Sl
No
Chapter
Must Know
Desirable to
Know
Long
Essay
Short
Essay
Short
Answer
I
Basic
Principles of
Medicinal
Chemistry
Physico-
chemical
properties of
drug
molecules
History and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
10 -- 2 12
II
Central
nervous
system
depressants
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR.
10 -- 2+2 14
III
Adrenergic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 2 7
IV
Cholinergic
drugs and
related agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
5 2+2 9
V
Local
anesthetics
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 5
VI
Histamine
and
antihistaminic
agents
Definition,
classification
with
structures
and synthesis
Histamine
structure,
biosynthesis
and biological
activity.
Histamine
- 5 2 7
10
receptors and
its actions
VII
Analgesic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR and
synthesis
.Steroidal
Antiinflammatar
y agents:
Cortisone,
Hydrocortison,
Dexamethasone
Betamethasone
Triamcinolone,
Fluocinolone
-- 5 2+2 9
VIII
Structure and
medicinal uses
of important
prostaglandin
s
Structure
and
medicinal
uses of
important
prostaglandi
ns
-- -- 2 2
IX
Natural
Products
Definition,
classification
with
structures
and synthesis
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
- 5 5
Total 20 30 20 70
* 80 % of the questions shall be from the Must Know area and 20 % shall be from the
Desirable to know area of the Curriculum.
11
6. Question paper layout to show which question number will represent which chapter (s)
Long Essay: 2X 10 = 20
1 Basic Principles of medicinal chemistry
2 Central nervous system depressant
Short Essays: 5x 6 = 30
3 Adrenergic drugs
4 Cholinergic drugs and related agents
5 Local anaesthetics
6 Histamine and antihistaminic agents
7 Analgesic agents
8 Natural products
Short Answers: 2X10 = 20
9 Basic Principles of medicinal chemistry
10 Central nervous system depressant
11 Central nervous system depressant
12 Adrenergic drugs
13 Cholinergic drugs and related agents
14 Cholinergic drugs and related agents
15 Histamine and antihistaminic agents
16 Analgesic agents
17 Analgesic agents
18 Structure and medicinal uses of important prostaglandins
7. Scheme of Practical / Clinical Teaching and Assessment:
List the expected practical / clinical competencies.
State the objectives for each competency.
Assign content for the objectives.
Describe the teaching ? learning processes.
Sl No Skills Duration Learning methods
1 Demonstrate the methods of
synthesis of simple organic
compounds used as drugs or
starting materials.
2 Demonstrate the various
methods of filtration,
crystallization, purification.
3 Reason critically and
logically and make
independent judgments
4 Employ scientific
12
methodologies such as
experimental design, and
the critical analysis of data
5 Interact effectively as part
of a team in order to work
towards a common outcome
7 Demonstrate an
understanding of the
chemical industry and the
way it operates, especially
the pharmaceutical industry
and others involving
synthesis such as the
petrochemical, polymer and
agrichemical industries
Scheme of examination with the distribution of marks as per the prioritisation of
competencies.
Sl No Competency Assessment criteria Marks
A Knowledge
B Cognitive and intellectual
skills
Synopsis 10
C Subject specific practical
skills
Major & Minor Experiment-I, Minor
experiment-II
25+15+10
D Transferable professional
skills
Viva-voce 10
Total 70
FirstRanker.com - FirstRanker's Choice
1
THIRD Year B. Pharmacy
1. Name of subject : MEDICINAL CHEMISTRY-I
2. Departmental objectives:
A. Learning Objectives:
i. To relate the structure and physical properties of drugs to their pharmacological
activity.
ii. To demonstrate an understanding of concepts such as drug metabolism,
bioavailability and pharmacokinetics and the role of medicinal chemistry in
improving these parameters.
iii. To understand the basic biological and pharmacological interactions by using
both natural products and synthetic bioactive molecules
iv. To learn about the characterization of drugs and drug-like molecules.
v. To understand principles of drug action and the role of bonding in drug-target
interactions, identification of targets for drug action.
vi. To describe the mechanism of action, synthesis and medicinal uses of different class
of chemotherapeutic agents.
vii. To differentiate drugs according to their action and give examples of each class of
drug.
viii. To describe the synthetic routes used to prepare some selected drug compounds.
ix. To understand simple methods of synthesis, purification and characterization of an
organic medicinal compound in the laboratory.
x. To train the students in basic & newer approaches in synthesis of drug molecules
chemical entities.
B. Learning Outcomes:
i. Learn the classification of chemotherapeutic agents based on their chemical group,
their mode of action and medicinal uses.
ii. Understands and describes the synthesis, structure activity relationships and mode
of action of drugs used in the treatment of diseases.
iii. Use of corresponding knowledge for the development of biologically and clinically
active drugs.
iv. Employ scientific methodologies such as experimental design, and the critical
analysis of data.
v. Based on a knowledge of the biochemical details for specific drug mechanisms, to
develop the ability to distinguish superior therapeutic drug mechanisms
vi. Describe the synthesis of important target compounds.
3. Annual objectives (for each year, if the subject is spread over different years): NA
2
4. Content distribution as per the list of topics, time allotted for each topic, distribution for
?Must know?, ?Desirable to know? and ?Nice to know? and the probable weightage.
Learning content distribution Sl
No
Topic Hours
Must know Desirable to
know
Nice
to
know
Weightage
(Marks)
I Basic
Principles
of
Medicinal
Chemistry
12 a) Effects of the following
physicochemical
properties of drug
molecules on biological
activity: Ionisation,
hydrogen bonding,
solubility, partition
coefficient, logP, logD,
protein binding,
chelation and polar
surface area.
b) Receptor and drug
receptor interactions.
c) Drug metabolism:
Biotransformation, sites
of biotransformation,
General pathways of
drug biotransformation,
role of cytochrome P-
450 and monoamino
oxygenase in oxidative
biotransformation,
oxidative, reductive,
hydrolytic and
conjugation reactions
with examples.
d) History
and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
15-16
A study of development of the following classes of drugs including structure activity relationship
(SAR), mechanism of action, synthesis of compounds superscribed by ?s?, chemical
nomenclature, generic names, brand names (a few important marketed products) and side effects.
II Central
nervous
system
depressants
16 A) General Anaesthetics:
Definition, mode of
action
Inhalation anaesthetics:
Halothane
s
,Nitrous oxide
Methoxyflurane,
1. Ultra shot acting
barbiturates:
Methohexitol sodium
s
,
2. Thiopental sodium
3. Dissociative
anaesthetics: Ketamine
HCl
20-21
3
B. Tranquilizers, sedatives
and hypnotics
1. Major tranquilizers:
SAR of Phenothiazines,
Promethazine HCl,
Chlorpromazine HCl
s
,
Prochlorperazine,
thioridazine HCl
Thioxanthenes:
clozapine,
Chlorprothixene,
thiothixine,
Fluorobutyrophenones:
Haloperidol
s
,
Resperidone
Beta amino ketones:
Molindone HCl,
Benzamaide surpieride
Minor tranquilizers:
SAR of Benzodiazepines,
Chlordiazepoxide,
Diazepam
s
, Orazepam,
Chlorazepam,
Lorazepam, Flurazepam,
Alprazolam
s
, Triazolam
s
2.Barbiturates:
Classification and SAR,
Barbital
s
, Methobarbital
s
,
Phenobarbital,
Amobarbital
s
, Butarbital,
Pentobarbital,
Secobarbital
3.Miscellaneous sedative
hypnotics:
a)Amides and imides:
Glutethimide
s
,
Methyprylon,
Methaqualone
s
b) Alcohols and their
carbamate derivatives:
Ethchlorvynol,
Ethinamate,
Meprobamate
s
c) Aldehydes and their
derivatives: Chloral
hydrate, Paraldehyde
C.Skeletal muscle
relaxants:
Chlorphenesin
s
,
Methocarbamol,
Chlorzoxazone
4
D. Drugs used in spasticity:
Baclofen, Buspirone
E.Anticonvulsants:
Structural requirement for
anticonvulsant activity,
mechanism of
anticonvulsant action
1.Barbiturates:
Phenobarbitone,
Mepobarbitone
2.Hydantoins:Phenytoin
s
,
Ethotoin, Mephenytoin
3.Oxazolidinediones:
Trimethadione
s
,
Paramethadione
4.Succinimides:
Phensuximide
s
,
Methsuximide,
Ethsuximide
5.Urea and monoacyl ureas:
Phenacemide,
Carbamazepine
s
6.Benzodiazepines:
Clonazepam
s
,
7.Miscellaneous: Primidone,
Valproic acid
III Adrenergic
agents
9 A.Adrenergic
Neurotransmitters and their
biosynthesis and metabolism,
adrenergic receptors their
distribution and actions
mediated by them
B. Sympathomimetics
1.Direct acting:
SAR, Endogenous
catecholamines,
a) Alpha adrenergic
agonists: Phenylephrine
s
,
Methoxamine,
Naphazoline,
Xylometazoline
s
,
Oxymetazoline,
Clonidine
s
, Guanabenz,
Methyldopa
b) Dual agonist/ antagonist:
Dobutamine
c) Beta adrenergic agonists:
Isoproterenol
s
,
Metaproterenol,
Terbutalin
s
, Albuterol,
11-12
5
Salbuterol, Bitolterol,
Ritodrine
2.Indirect acting:
Hydroxyamphetamine,
Propylhexedrine
3. Mixed acting: Ephedrine,
Metaraminol
C. Adrenolytics:
1. Alpha blockers:
a) Non selective: Tolazoline
b) Irreversible blockers:
Phenoxybenzamine
s
c) Alpha
1
blockers:
Prazosin
s
, Doxazosin,
Tamsulosin
d) Alpha
2
blockers:
Yohimbine, Coryanthine
2. Beta blockers: SAR
a) Non selective blockers:
Propranolol
s
, Nadolol,
Pindolol, Timolol, Sotalol
b) Beta
1
blockers:
Acebutolol, Atenelol,
Esmolol, Metaprolol
s
c) Betablockers with alpha
1
antagonistic activity:
Labetalol, Carvedilol
IV Cholinergic
drugs and
related
agents
12 1.Cholinergic
neurotransmitter:
Biosynthesis, metabolism
and functions of
acetylcholine
2.Cholinergic receptors:
Nicotinic, muscarinic and
their subtypes
A. Cholinergic agonists:
1.Stereochemistry and
SAR, Acetylcholine,
Methacholine, Carbachol,
Bethanechol, Pilocarpine
2. Cholesterase inhibitors:
a) Reversible: Mode of
action, Physostigmine,
Neostigmine
s
,
Ambenonium,
Demecarium,
Edrophonium, Tacrine
b) Irreversible: Mode of
15-16
6
action, Isoflurophate,
Ecothiophate,
Malathion, Parathion,
Pralidoxime.
B.Cholinergic blockers:
SAR
1.Postganglionic blockers:
Structural considerations
of solanaceous alkaloids
and analogs, Atropine,
Hyoscyamine,
Scopolamine,
Homatropine, Ipratropium
2.Synthetic agents:
Clidinium, Dicyclomine
s
,
Glycopyrrolate,
Methantheline,
Propantheline,
Benztropine, Procyclidine,
Tropicamide
s
3.Ganglionic blockers: Mode
of action, Trimethaphan,
Mecamylamine
4.Neuromuscular blockers:
Mode of action,
Tubocurarine, Metocurine,
Gallamine,
Pancuronium,
Vecuronium.
V Local
anesthetics
4 A. Definition, classification,
and mechanism of action
B. SAR of lidocaine
derivatives
C. 1. Benzoic acid
derivatives: Hexylcaine,
Cyclomethicaine,
Piperocaine.
2. Aminobenzoic acid
derivatives:
Benzocaine, Procaine s,
Procainamide
3. Lidocaine derivatives
(Anilides):
Lidocaines, Prilocaine
4. Miscellaneous:
Dimethisoquin,
Dibucaine
5-6
7
VI Histamine
and
antihistami
nic agents
6 B. Antihistaminics:
H1 antagonists
a) Aminoalkyl ethers:
Diphenhydramine
HCl,
Bromodiphenhydrami
ne, Doxylamine
b) Ethylene diamines:
Tripelenamine
,
Pyrilamine
c) Propylamine
derivatives:
Pheniramine,
Chlorpheniramine
s
d) Phenothiazine
derivatives:
Promethazine
s
,
Trimeprazine
e) Piperazine derivatives:
Cyclizine, Meclizine,
Cetrizine
s
f) Miscellaneous
compounds:
Phenindamine,
Cyproheptadine
C.H
2
Antagonists:
Mechanism, Cimetidine,
Ranitidine, Famotidine
D. Gastric proton pump
inhibitors: Mechanism of
action, Omeprazole
s
,
Pentaprazole, Rabiprazole,
Lansoprazole.
A.
Histamine:
receptors and
its actions
8-9
VII Analgesic
agents
9 A. 1. Narcotic analgesics:
Opoid receptors, SAR,
Morphine, Codiene,
Diacetylmorphine,
Levorphanol,
Dextromethorphan
s
,
Pentazocine, Meperidine,
Loperamide, Fentanyl,
Methadone
s
,
Propoxyphene, Tramadol
2. Narcotic antagonists:
Butorphanol, Nalorphine,
Levalorphan, Naltrexone,
Naloxone
B. Non narcotic analgesics:
2.Non steroidal anti-
inflammatory agents:
Mechanism of action
1.Steroidal
Antiinflammator
agents:
Cortisone,
Hydrocortisone,
Dexamethasone,
Betamethasone,
Triamcinolone,
Fluocinolone
11-12
8
a) Salicylic acid
derivatives: Aspirin
b) N-aryl anthranilic acid
derivatives: Mefenamic
acid
s
, Diclofenac,
Aceclofenac
c) Aryl acetic acid
derivatives:
Indomethacin,
Ibuprofen
s
, Piroxicam
s
,
Naproxen
s
d) Aniline and
paraaminophenol
derivatives: Phenacetin,
Acetaminophen
s
e) Pyrazolone and
pyrazolidine dione
derivatives: Antipyrin,
Oxyphenbutazone,
Phenylbutazone
f) Diaryl sulphonamides:
Nimesulide
s
, Rofecoxib,
Valdecoxib
VII Structure
and
medicinal
uses of
important
prostaglan
dins
1 Structure and medicinal uses
of important prostaglandins
1-2
IX Natural
Products
6 A. Alkaloids: Definition,
Classification,
B. Purines:
Definition, Interrelation
among caffeine,
theophylline, theobromine
C. Terpenoids: Definition,
classification, isoprene and
special isoprene rule,
Interrelationship among
monocyclic monoterpenoids
like limonene, dipentene,
alphaterpenoid, alpha
terpenion, terpenolene,
terpin, terpene hydrate,
carvone and cineone.
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
8-9
9
5. Blueprint of question paper, for each QP..
Marks distribution
Total
Marks
Sl
No
Chapter
Must Know
Desirable to
Know
Long
Essay
Short
Essay
Short
Answer
I
Basic
Principles of
Medicinal
Chemistry
Physico-
chemical
properties of
drug
molecules
History and
development
of Medicinal
Chemistry,
definition of
hit, lead and
drug.
10 -- 2 12
II
Central
nervous
system
depressants
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR.
10 -- 2+2 14
III
Adrenergic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 2 7
IV
Cholinergic
drugs and
related agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
5 2+2 9
V
Local
anesthetics
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR
- 5 5
VI
Histamine
and
antihistaminic
agents
Definition,
classification
with
structures
and synthesis
Histamine
structure,
biosynthesis
and biological
activity.
Histamine
- 5 2 7
10
receptors and
its actions
VII
Analgesic
agents
Definition,
Mechanism
of action,
classification
with
structures
and synthesis
SAR and
synthesis
.Steroidal
Antiinflammatar
y agents:
Cortisone,
Hydrocortison,
Dexamethasone
Betamethasone
Triamcinolone,
Fluocinolone
-- 5 2+2 9
VIII
Structure and
medicinal uses
of important
prostaglandin
s
Structure
and
medicinal
uses of
important
prostaglandi
ns
-- -- 2 2
IX
Natural
Products
Definition,
classification
with
structures
and synthesis
Structural
elucidation of
ephedrine.
Structural
elucidation of
caffeine,
- 5 5
Total 20 30 20 70
* 80 % of the questions shall be from the Must Know area and 20 % shall be from the
Desirable to know area of the Curriculum.
11
6. Question paper layout to show which question number will represent which chapter (s)
Long Essay: 2X 10 = 20
1 Basic Principles of medicinal chemistry
2 Central nervous system depressant
Short Essays: 5x 6 = 30
3 Adrenergic drugs
4 Cholinergic drugs and related agents
5 Local anaesthetics
6 Histamine and antihistaminic agents
7 Analgesic agents
8 Natural products
Short Answers: 2X10 = 20
9 Basic Principles of medicinal chemistry
10 Central nervous system depressant
11 Central nervous system depressant
12 Adrenergic drugs
13 Cholinergic drugs and related agents
14 Cholinergic drugs and related agents
15 Histamine and antihistaminic agents
16 Analgesic agents
17 Analgesic agents
18 Structure and medicinal uses of important prostaglandins
7. Scheme of Practical / Clinical Teaching and Assessment:
List the expected practical / clinical competencies.
State the objectives for each competency.
Assign content for the objectives.
Describe the teaching ? learning processes.
Sl No Skills Duration Learning methods
1 Demonstrate the methods of
synthesis of simple organic
compounds used as drugs or
starting materials.
2 Demonstrate the various
methods of filtration,
crystallization, purification.
3 Reason critically and
logically and make
independent judgments
4 Employ scientific
12
methodologies such as
experimental design, and
the critical analysis of data
5 Interact effectively as part
of a team in order to work
towards a common outcome
7 Demonstrate an
understanding of the
chemical industry and the
way it operates, especially
the pharmaceutical industry
and others involving
synthesis such as the
petrochemical, polymer and
agrichemical industries
Scheme of examination with the distribution of marks as per the prioritisation of
competencies.
Sl No Competency Assessment criteria Marks
A Knowledge
B Cognitive and intellectual
skills
Synopsis 10
C Subject specific practical
skills
Major & Minor Experiment-I, Minor
experiment-II
25+15+10
D Transferable professional
skills
Viva-voce 10
Total 70
13
8. Suggested references (as per Vancouver style):
? Basic references
? Advanced references (may also include journals / web / other electronic sources)
MEDICINAL CHEMISTRY II TEXT BOOKS (THEORY)
Latest editions and all volumes of
1. Foye's principles of Medicinal chemistry
2. Wilson and Griswold?s Text book of Organic and Pharmaceutical chemistry
3. Rama Rao Nadendla, Medicinal Chemistry
MEDICINAL CHEMISTRY II REFERENCE BOOKS (THEORY)
Latest editions and all volumes of
1. Burger's medicinal chemistry
2. The Martindale's Extra Pharmacopoeia
3. A.I.Vogel, Text Book of practical organic chemistry including the qualitative analysis
4. A.H.Becket and J.B.Stanlake, Practical Pharmaceutical chemistry
5. M Raghuprasad, Advanced medicinal chemistry: A laboratory guide
6. J.G.Mann and Saunders, Practical organic chemistry, ELBS Longman, London
7. I.P.1985, Ministry of Health, Govt. of India
8. LedniserMitzsher, Organic drug synthesis, Vol.1 and 2
9. I.L. Finar, Text Book organic chemistry
10. T. Robinson, Organic constituents of higher plants
11. Feiser and Feiser Steroids
12. Drug design by Ariens
13. Smith and Williams, Introduction to principles of drug design
14. Purcell, Strategy of drug design
15. CIMS
MEDICINAL CHEMISTRY II REFERENCE BOOKS (PRACTICALS)
1. A.I.Vogel, Text Book of practical organic chemistry
2. A.H. Beckett and Stanlake, Practical pharmaceutical chemistry
3. J.G.Mann and Saunders, Practical organic chemistry
4. Jayaveera KN, Practical medicinal chemistry
5. Raghuprasad M, Advanced medicinal Chemistry
6. Feiser and Feiser, Steroids
7. IP 1985
8. I.L.Finar, Textbook of organic chemistry
9. CIMS
FirstRanker.com - FirstRanker's Choice
This post was last modified on 02 March 2020