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APPENDIX
-
II



SYLLABUS


M.Sc. PHARMACEUTICAL CHEMISTRY





PART
-
II


Examinations for 20
11
-
12 &
20
12
-
13
Session
s


OUTLINES OF THE TEST

The examination will consist of two semesters in the second year i.e. semester III and IV.
In the III semester
there shall be 4 theory papers and 2 practical papers. In the IV semester,
there shall be t
hree

theory papers and one practical paper. In addition, the students shall
under take project work on research/Industrial problems. Each theory paper shall be of 10
0
marks of which 75 marks shall be allocated to the Theory Paper set by external examiner.
The
internal assessment

in each paper shall have 25 marks. There shall be two assignments
of 5 marks each, one test of 10 marks (best of two shall be taken) and 5 ma
rks for seminar.






SEMESTER
-
II
I (November/December)



Paper


Title of paper







Marks


Theory IX


Medicinal Chemistry

I





100


X


New Drug Development & Toxicology



100


XI


Pharmaceutical Tech
nology
-
I





100


XII


Drug Design and Drug Development


I



100


Practical V


Analysis of Pharmaceuticals





100




VI


Formulation of dosage forms





100




Total








600





SEMESTER
-
I
V

(
April/May)



Paper


Title of paper







Marks


Theory XIII


Medicinal Chemistry
-
II





100


XIV


Drug Design & Drug Development
-
I
I




100


XV


Pharma
ceutical

Technology
-
II




100

Practical
-
VII


Sy
nthetic Medicinal Chemistry




100




Project work







2
00




Total








600
















M.Sc PHARMACEUTICAL CHEMISTRY


(SE
MESTER
-
III)


PAPER
-
IX: MEDIC
IN
AL CHEM
I
STRY

I

Time: 3 hours









Max Marks: 75









Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper w
ill consist of five sections A, B, C, D and E. Section A, B, C and D
will have two questions from the respective sections of the syllabus and carry 12 marks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus
uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:


1.

Candidates are required to attempt one question each from sections A, B, C and D



of the question paper and the entire section E.


SECTION
-
A


i
.

Introduction to Ph
armaceuticals, Historical development, Classification of
drugs,



N
omenclature of Pharmaceuticals &
Drug metabolism reactions.

ii.
Structure,



stereochemistry,


nomenclature,



mode of action,



specific

clinical





applications and

structure activity relationships
,

biosynthesis of naturally occurring


compounds
and

synthesis of prototypical drugs in each category (Chemical &


Pharmacological) for the
following classes of drugs.



Hormones:

Sex


hormones


and


related


compounds


(Estrogens,


Androgens,


Progestational

agents,


Anabolic


steroids,


Contraceptives),

Adrenal cortex


hormones,

Thyroid


hormones


and


antithyroid


drugs,


pancreatic


hormones,




Hypothalamus

hormon
es.



Vitamin
s:


Fat soluble vitamins (
A, D, E and K) , water soluble vitamins (Folic



acid
,

B
12

and C).


Adrenergic

and


cholinergic


drugs
(Agonist & antagonists)
:





Sympathomimetics,


Catecholamines,

Phenylethamolamine
s, Phenylethlamines,


Non
-
catecholamines, Imidazoline

derivatives, Adrenergic blocking agents.


Cholinergic agents:

Autonomic blocking and related
drugs. Antispasmodic and


antiulcer drugs. Antiparkinsonism drugs.


SECTION
-
B

Structu
re, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypical drugs in each category (Chemical & Pharmacological)

for the
following classes of drugs.


Cardiovascular
drugs:
Vasodilators, Antihypertensive agents,

A
ntihypercholesterolemic
drugs, Antiarrhythmic drugs, Sclerosing agents, Coagulants and anticoagulants,
Cardiotonic compounds,
Cardiac glycosider & inotropic a
gents

Synthetic hypoglycemic

agents.

Diuretics
:

Osmotic agents, Acidfying salts
,

Mercurials, Purines and related
heterocycles
,

Sulfonamides, Benzothiadiazene and related compounds, Chloroth
i
azides and analogs.
Sulfamoylebenzoic acid and analogs, Endocrine

A
ntagonists
,

Miscellan
e
ous diuretics.



SECTION
-
C

Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypic
al drugs in each category (Chemical & Pharmacological) for the
following classes of drugs.


General


Anesthetics:

Theories of Gener
al Anesthetics, Ethers,

Halogenated
hydrocarbo
ns, Cyclopropane, Nitrous oxide, Barbiturates,

Adjuncts

to general anesthe
tics,
metabolism of volatile anesthetics.

Local anesthetics:

Cocoa alkaloids


Cocaine and Synthetic compounds, Esters, Amides,
Miscellaneous anesthetics.

C
NS Active Drugs:
CNS Depressants:

Hypnotics and sedatives
: Barbiturates, Non
barbiturates, Amides a
nd Imides,

Bezodiazepines, Aldehydes and derivatives,
Methaqualone and other miscellaneous agents. Anticonvulsants: Barbiturates, Hydanato
i
ns.
Oxazolidinediones. Succinmides, Bezodiazepines, Thenacemide,
G
lutethimide
.

CNS
-
stimulants & Psychoactive drugs:
Ana
leptics, Purines, Psyschomotor stimulants,
Sympathomimetics, Monamine oxidase Inhibitors. Tricyclic antidepressants, Miscellaneous
psychomotor stimulants.
Hallucinogens (Psychodelics, Psychomimetics):
Indolethylamines,

ß
-
phenylethylamines, Butyrophenone
s and other miscellaneous drugs.


SECTION
-
D

Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypical dr
ugs in each category (Chemical & Pharmacological) for the
following classes of drugs.


A
nalgesics and Antitussives:

Morphine and related opioids, Narcotic antagonists,
Synthetic analgesics
-

Antitussives: Opium alkaloid, Morphine analogs, Synthetic non
-
n
arcotic antitussives,
m
ucolyt
ic

agents.

Antipyretics and Non
-
steroidal Anti
-
inflammatory agents:

Salicyclic acid

derivatives.
Indolyl and Arylacetic acid derivatives. Pyrazole derivatives. Aminophenol derivatives,
Arylpropionic acid derivatives, Salol Pri
nciple, Anti
-

Gout Drugs.

Antiallergics:

Serotonin, Bradykinin, Antihistamines (ethylenediamine derivatives of
aminoalkyl ethers, derivatives of cyclic basic chains, Monoaminopropy
l

derivatives ,
Derivatives of tricyclic compounds
)
.

Radio Pharmaceuticals:

Pharmaceutical examples for therapeutic & diagnostic agents
Precautions & safety measures for handling & disposing.


Books Recommended:

1
.

Wilson and Gisvolds Textbook of Organic Medicinal and
Pharmaceuticals



Chemistry, 8
th

edition, edited
by R.F. Doerge, J.B. Lippincott Company,


Philade
l
phia, 1982.

2.

Pharmaceutical Chemicals in Perspective, B.G. Reuben and H.A. Wittcoff, John




Wiley & Sons, New York, 1989.

3.

W.C. Foye, Principles of Medicinal Chemistry, Lea & Febige
r, Philadelphia,


U.S.A.

Suggested
Readings
:

Strategies for Organic Drug Synthesis and Design, D.Lendnicer, John Wiley and Son, New
York, 1998.



M.Sc PHARMACEUTICAL CHEMISTRY


(SEMESTER
-
III)


PAPER
-
X:
NEW DRUG DEVELOPMENT AND TOXICOLOGY


Time:

3 hours









Max Marks: 75









Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Section A, B, C and D
will h
ave two questions from the respective sections of the syllabus and carry 12 marks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:

Candid
ates are required to attempt one question each from sections A, B, C and D of the
question paper and the entire section E.


SECTION
-
A

Common laboratory animals in pharmacology research, regulations for the ca
re

and use of
laboratory animals.

Preclinical

safety evaluation of new chemical agent :

Concept of

LD
50
, Determination of
LD
50
, acute, sub
-
chro
n
ic and chro
n
ic toxicity studies.


SECTION
-
B

Clinical
evaluation of new chemical entity : Placebo, clinical trial study designs, phase of
clinical trials.

B
io assays: Basic principles of bio
-
assays, types of bioassays and application.

-

RIA : Principles of R
I
A

and application.

-

ELISA : Principles and application.


SECTION
-
C

Toxicology : General principles of management of poisoning.
Diagnosis and
Management
of

t
oxicity due to atropine, barbiturates , Mor
ph
in
e &

A
lcohol.


SECTION
-
D

Experimental models to screen the following class
es

of drugs:
-

-
Analgesics

-

Anti
-
inflammatory agents.

-

Anti
-

psychotics

-

Anti
-

depressants

-

Anti
-
anxiety agents

-

Anti
-
ulcer dru
gs

-

Anti
-
diabetics






BOOKS RECOMMENDED

1.

F.C.Lu, Basic Toxicology : Fundamentals, Target Organs and Risk Assessment , 3
rd



edition, Taylor and Francis, Washington, U.S.A. 1996.

2.

D.R. Laurence and A.L. Bachrach, (eds.) Evaluation of Drug
activities


Pharmnacometrics Vol. I, Academic Press, London, U.K. 1964.

3.

M.N. Ghosh, Fundamentals of Experimental Pharmacology, 2
nd

edition , Scientific



Book Agency, Calcutta, India, 1984.

4.

H.G. Vogel and W.H. Vogel (eds.) , Dru
g Discovery and Evaluation
-


Pharmacological Assays, Sp
ringer Verlag, Berlin, Germany,1997.






























M.Sc PHARMACEUTICAL CHEMISTRY

(SEMESTER
-
I
II
)


PAPER
-
X
I
:
PHARMACE
UTICAL TECHNOLOGY
-
I

Time: 3 hours









Max Marks: 75









Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Sec
tion A, B, C and D
will have two questions from the respective sections of the syllabus and carry 12 marks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS F
OR THE CANDIDATES:

1.

Candidates are required to attempt one question each from sections A, B, C and D


of the question paper and the entire section E.

2.

The use of non
programmable

calculators is allowed.


SECTION
-
A

i. Introduction t
o different Pharmaceutical dosage
forms, with

their
advantages

&



li
mitations, organoleptic additives and stabilizing agents (dyes,
l
akes, f
l
avo
ur
s,




suspending
agents
, emulsifying agents, anti oxida
n
ts, preservatives etc) used in




pharmaceutical dosage forms.

ii.

Preformulation considerations:
Need for pre
fo
rmulation studies, methods used


for assessing drug
-
excipient interactions, Importance of physic
o
-
chemical properties


of drug in dosage form de
velopment (pH, pKa, partition

co
efficient etc
)
.



SECTION
-
B

Processing of tablets:

Advantages and disadvantages of tablets, types of tablets.
Granulation
-

dry
,

wet and direct compression. Basic characteristics and properties of
excipients used in different

types of granulation
processes
. Various additives used in tablet
formulations.


Compression of tablet
-

compressing machines and their tooling, processing problems and
their remedy. Evaluation of tablets as per official standards.

Tablet coating:

Coating p
rinciples and equipment, Coating processes
-
sugar coating, Film
coating and enteric coating. Materials used in coating.

F
ilm characteristics,
defects

and their
remedies. Evaluation of coated tablets.


SECTION
-
C

Processing of Capsules:

Hard gelatin capsules
-

Materials and production . Filling
equipment, hand filling, semiautomatic and automatic filling. Operations, formulation.
Finishing and evaluation.


Soft gelatin capsule
-
manufacture process, nature of capsule shell and contents. Evaluation,
physical stabi
lity and packing.

Microencapsulation:

Importance and applications of microencapsulation in Pharmacy.
Various techniques and equipment employed for microencapsulation.



SECTION
-
D

Liquid dosage forms:

Types, advantages and disadvantages.

a.

Monophasic liqu
id dosage forms
:

Techniques of increasing solubility of


drugs, other problems involved in preparation and stability of liquids.


b.

Biphasic liquid dosage forms
:


i.

Suspensions
: Preparation and evaluation of suspensions, stability testing.



Problems in suspension formulation, flocculated and non
-
flocculated


suspensions.

ii.


Emulsions
: Advantages of emulsion dosage form, types, identification,


selection of emulsifying agents. Preparation
, Calculation of HLB value


and stability studies.


Semi
-

Solid dosage forms:

Types of semi
-
solid dosage forms ointments, creams

and suppositories. Bases used in their preparation and their characteristics. Brief discussion
o
n

their evaluati
on.


Books Recommended:

1.

C.W. Copper and G. Gunn, Dispensing Pharmacy, CBS Publishers &


Distributors, Delhi
-
110032.

2.

L.Lachman et. al., Theory and Practice of Industrial Pharmacy, Varghese


Publishing House, Dadar, Bombay
-
4000
14,1987.


Suggested
Readings
s:

1.


A.Osol Remington’s Pharmaceutical Sciences, XVIII edition, Mack


Publishing co., Pennsylvania, USA, 1990.

2.

The Pharmacopoeia of India. IIIrd Edition, Vol. I and Vol. II, 1996, Govt. of


India, Mini
stry of Health and Family Welfare Delhi.

3.

British Pharmacopoeia, International Edition, 1993.

4.

The United States Pharmacopoeia, XXII & NF XVII and addenda, 1995.

5.

The Pharmaceutical Codex, 12
th

Edition, The Pharmaceutical Press, London,



1994.

6.

Patrick B. Deasy , Microencapsulation and related drug processes, Dekker series


Vol.20.

7.

F.J.R. Nixon, Microencapsulation, Dekker series Vol 3.

8.

Joseph R. Robinson, Sustained and Controlled Drug Delivery Systems, Dekker



Series. Vol. 6.











M.Sc PHARMACEUTICAL CHEMISTRY


(SEMESTER
-
I
II
)

PAPER
-
X
II
:

DRUG DESIGN AND DRUG DEVELOPMENT
-
I

Time: 3 hours









Max Mark
s: 75









Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Section A, B, C and D
will have two questions from the respective sections

of the syllabus and carry 12 marks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:

1.

Candidates are required to attempt one question e
ach from sections A, B, C and D


of the question paper and the entire section E.

2.

The use of scientific calculators is allowed.


SECTION
-
A


Introduction to Drug Design & Drug Development

: Definition, History (Chronological
Evolution), Drug d
esign approaches, Lead optimization, de Novo drug design.

Quantum Mechanics:

Introduction to quantum mechanics, postulates of quantum
mechanics, Schrodinger equation , Perturbation theories of drug action, Pullman’s
dipositive bond theory , Role of charge

transfer process in drug action, conformational
aspects & molecular orbital calculations , molecular orbital approach to drug design with
examples.


SECTION
-
B


Drug Receptor Interactions:
Historical background, Receptor theories, Forces involved in
drug

receptor interactions; covalent & non
-
covalent interactions ; Agonist &

antagonists.

QSAR Analysis :

Parameters & Biological data for QSAR,

Design of Test series in
QSAR:

Craig plot, T
o
plis
s

operational scheme, cluster analysis.

Quantitativ
e

models:
Hansch (Extrathermodynamic) , Free Wilson (Additivity model) , Mixed approach.

Statistical method for QSAR:

Regression analysis, multiple regression, stepwise multiple
regression, Partial least square analysis. Validation of QSAR models.


SECTION
-
C

Pharmacokinetics in
D
rug designing:

Pharmacokinetics, Environmental
pharmacokinetics. Single and two compartment pharmacokinetics. Pharmacokinetics of
drug metabolism. Dissection of a drug molecule in to biofunctional moieties. Modulation
of ph
armacokinetics by molecular manipulations, Modulation of distribution of pharmacea
over various compartments, Modulation of time
-
concentration relationship . Lipinski Rule,
QSPR, Biopharmaceutics. Generic equivalence and non
-
equivalence. Role of
biopharmac
eutics in Drug designing.




SECTION
-
D


Peptidomimetics:

Peptidomimetics research, Rational design of Peptidomimetics,
nonpeptide, Ligands for peptide receptors, Applications of oligonucleotides in antiviral and
antitumoral chemotherapy. Antisense nucleot
ides designing. Carbohydrate based
Therapeutics
.


Prodrug Approach:

Basic concept, Common promoities. Reversal of prodrugs
-

chemical
and enzymatic . Application of prodrug approach to alter taste and odour, reduction of pain
at injection site, reduction of

gastrointestinal irritability. Alteration of drug solubility,
increasing chemical stability. Prevention of presystematic metabolism. Prolongation of
drug action, Site spectic drug delivery. Reduction in drug toxicity. Alteration of drug
metabolism.


Books

Recommended:

1.

The Organic Chemistry of Drug Design and Drug Action. by R.B. Silverman,


Academic Press,1992.

2.

Drug Designs
-

A series of monographs in medicinal chemistry edited by A.J.


Ariens. Ist edition. Vol. I, II, V, VIII &
IX (only relevant chapters).

3.

Comprehensive medicinal chemistry. Peragmon Press. 1990, Vol.4.

4.


Burger’s Medicinal Chemistry & Drug Discovery . fifth edition vol
-
.I, Willey


Interscience.


Suggested
Readings
s:

1.

Medicinal Chemistry fo
r 21
st

century edited by C.G. Wermuth, Blackwell


Scientific Publications, 1997.






















M. Sc. PHARMACEUTICAL CHEMISTRY


(SEMESTER
-
I
II
)


Practical Paper
-

V : Analysis of Pharmaceutical


Time: 4 hours



M. marks: 100













Total practical hours: 60

Suggested Experiments


1.

Separation of components of APC by TLC.
1
HNMR & IR analysis of its components.

2.

Qualitat
ive applications of ultra
-
violet spectroscopy.

3.

Quantitative application of infrared spectroscopy.

4.

Determination of molecular weight by .
1
HNMR

5.

Structural isomer identification by.
1
HNMR.

6.

Analysis of benzene traces in alcohol, homologous benzene derivatives
and amino acids by
high order derivatives UV spectroscopy.

7.

Determination of water content by moisture balance and by Karl Fischer method.

8.

Measurement of Specific Optical Rotation of ibuprofen and determination of unknown
concentration.

9.

Volumetric analysis
of ibuprofen in tablets.

10.

Analysis of ascorbic acid in given tablets.

11.

Spectrophotometric determination of aspirin content in soluble aspirin tablets.

12.

Spectrophotometric determination of Paracetamol in tablets.

13.

Extraction of oxyphenyl butazone from tablets.
Its spectrophotometric analysis.

14.

Analysis of Ampicillin trihydrate.

15.

Analysis of Dextrose.

16.

Extraction of cholesterol from Gall Stones and its analysis.

17.

Analysis of citric acid.

18.

Determination of Vitamin B
1

in given tablets.

19.

Determination of vitamin B
2
in giv
en tablets.

20.

Determination of ephedrine hydrochloride in given syrup.

21.

Determination of tetracycline in given capsules.

22.

Determination of phenobarbitone in given cough syrup

23.

Determination of chloremphenicol in given capsules

24.

To perform I.P. monograph of table
ts.

25.

To perform I.P. monograph of hard gelatin capsules.

26.

Evaluation of injections (ampoules 2 ml. and 5 ml.)

27.

In


vitro comparative study of the release and penetration of drugs from topical
preparations.

28.

Evaluation of sustained release oral formulation (s)
.

29.

To study the dissolution rate of nitrofurantion /aspirin tablets.

30.

Determination of activity of enzyme penicillin.

31.

Analysis of activated charcoal.

32.

To perform quality control tests on surgical gauge Bandage cotton.

Note
: Any other experiment (s) may be inc
luded in support of the theoretical aspects of the
course.





M. Sc. PHARMACEUTICAL CHEMISTRY



(SEMESTER
-
I
II
)



Practical Paper
-

VI : Formulation of dosage forms


Ti
me: 4 hours M. marks: 100











Total practical hours: 60


Suggested Experiments


1.

Preparation of effervescent granules.

2.

Preparation of cough syrup.

3.

Fo
rmulation of tablet of Paracetamol.

4.

Formulation of tablet of sodium bicarbonate.

5.

Preparation of capsule each containing 250mg of tetracycline.

6.

Preparation of microcapsule of methyl salicylate of polymer polymer interaction.

7.

Preparation of Antacid suspensio
n

8.

Preparation of vanishing cream (water based cream)

9.

Preparation of liquid paraffin emulsion

10.

Preparation of sunscreen cream

11.

Preparation of phenobarbitone elixir.

12.

Preparation of film coating of tablets.

13.

Preparation of enteric coating of tablets.

14.

Preparat
ion of antidandruff shampoo.

15.

Preparation of cold cream (Oil based cream)

16.

Preparation of non staining iodine ointment.

17.

Formulation of lubricating jelly.

18.

Formulation & preparation of deodorants /
antiperspirants
.

19.

Formulation & preparation of shaving crea
m.

20.

Formulation & preparation of lipsticks.

21.

Formulation & preparation of nail enamel.

22.

Formulation & preparation of after shave lotion.

23.

Formulation & preparation of calamine lotion.

24.

Formulation & preparation of mouth washes.



Note
: Any other experime
nt (s) may be included in support of the theoretical aspect of


course.









M.Sc PHARMACEUTICAL CHEMISTRY

(SEMESTER
-
I
V
)

PAPER
-
X
II
I
: MEDIC
IN
AL CHEM
I
STRY

I
I

Time: 3 hours









Max Marks: 75










Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Section A, B, C and D
will have two questions from the respective sections of the syllabus and carry 12 marks
eac
h. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:

Candidates are required to attempt one question each from sections A, B, C and D of
the que
stion paper and the entire section E.


SECTION
-
A

Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypica
l drugs in each category (Chemical & Pharmacological) for the
following classes of drugs.


A
ntibacterials:

Penicillines, Cephalosporins, Tetracyclines, Aminoglycosides,
Chloramphenicol, Macrolides, Lincomycins, Polypeptide antibiotics, Polyene antibiot
ics.
Sulfonamides and Sulfones
,

fluoroquinolines, Trimethoprim and other unclassified
antibiotics
.


A
ntimycobacterials:

Sulfanilamides, p
-
Aminosalicyclic acid derivatives , Thioamides,
Thiourea derivatives, Thiosemicarbonazones, Isoniazid, Kanamycin sulfat
e, Capreomycin,
Rifampin, Pyrazinamide, Anthionamide, Clofazimine, Cyclosporin, Dapsone, Sulfazem.

&
Antileprotic agents.


SECTION
-
B

Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relatio
nship
s
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypical drugs in each category (Chemical & Pharmacological) for the
following classes of drugs.


Anthelmintics:

Introduction. Tetrachloroethylene, Piperazines, Gentian viole
t, Pyr
a
n
tel

pamoate, Thiabendazole, Mabendazole, baphenium hydroxynaphthoate, Dichlophene,
Niclosamide, levamisole hydrochloride, Tetramisole, Niridazole, Biothional,
Antimonypotassium tartarate, Stibiophen, Sodium Stibiocaptate.


Antiamoebic and antiproto
zoal drugs:

Emetine hydrochloride, 8
-
Hydrox
y
quinoline,
Iodochlorohydroxyquinol, Metronidazole, Diloxanide furoate, Bilamical hydrochloride,
Hydroxysti
l
bamidine isothinate, Pentamidine isothionate, Nifurtimox, Suramin sodium,
Carbarsone, Glycobiarsol, Melar
soprol, Sodium stibogluconate, Dimercaprool,
Diethycarbamazine citrate, Centarsone, Acetarsone, Antimony potassium tartarate,
Bismuth sodium thioglycollate, Sulphonamide, Stibiophen, Bismuth sodium
thioglycollamate, Furazolidone.




SE
CTION
-
C

Structure, s
tereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships
,

biosynthesis of naturally occurring compounds
and

synthesis of prototypical drugs in each category (Chemical & Pharmacological) for t
he
following classes of drugs.


Antiviral agents:

Introduction, Screening methodology, Admantane derivatives
(Amantadine, Rimantadine), Idozuridine, Trifluridine, Vidarabine, Ribavarain,
Acycloguanosine, Inospiplex, Methisazone, Zidovudine, Acyclovir, Ganc
iclovir, Foscarnet,
Human interferon.

Antineoplastic agents:

Alkylating agents (Nitrogen mustards, Aziridines, Sulfonic acid
Esters, Epoxides, Nitrosoureas, Triazenes, Phosphamides, Mitomycin, comparative activity
of alky
la
ting agents).
Antimetaboilities:

Antifolates (Methotrexate), Mercap
t
opurine,
Thioguanine, fluorouracil, Flo
x
uridine, Cytarabine, Azathioprine, antitumor, antibiotics,
Dactinomycin, Daunorubricin, Aclacinomycin, Mithramycin, Bleomycin,
Miscellaneous
compounds:

C
i
splatin, Taxol, Gunazole,
Pipobromin,
Antitumor alkaloids:

Vincristine
,vinblastin.

Hormones agonist and a
nt
gonists:

Steroids, Tamoxifen, Mitotane,
Dromastanolone propionate, Testalactone, Megastrol acetate Immunotherapy.


SECTION
-
D

Structure, stereochemistry, nomenclature, mode of
action, specific clinical applications
and structure activity relationships
,
biosynthesis of naturally occurring compounds
and
synth
sis of prototypical drugs in each category (Chemical & Pharmacological) for the
following classes of drugs.


Antimala
rials:

Cinchona alkaloids, 4
-
Aminoquinolines, 8
-
Aminoquinolines,


9
-
Aminoacridines, Biguanides, Pyramidines.
Sulfones, Mefloquine and Sulfonamides.

Antifungal drugs:

Fatty acids and their derivatives (Propionic acid, zinc propionate,
sodium ca
prylate, zinc caprylate, undecylenic acid, Zinc undecylenate, Triacetin) .
Salicylanilids, Salicyclic acid, Tolnaftate, p
-
chloromethoxylenol, Acrisocrin, Fluconazole,
Itraconazole, Haloprogin, Clotrimazole, Econazole, Miconazole,
Ketoconazole,Flucytosine,
Griseofulvin, Polyene antibiotics (Nystatin, Amphoetericin
-
B),
Chlorophenesin, Dithranol.

Diagnostic Agents and Organic Pharmaceutical Aids:

Diagnostic agents:
Introduction,


Radiopharmaceuticals, Pharmacopoeia
l

examples of therapeutic & diagnostic agents
.
Precaut
ion

& safety measures for handling & disposing.


Books Recommended:

1.

Wilson and Gisvolds Textbook of Organic Medicinal and Pharmaceuticals


Chemistry, 8
th

edition, edited by R.F. Deorge, J.B. Lippincott Company,


Philadel
phia, 1982.

2.

Pharmaceutical Chemicals in Perspective. B.G. reuben and H.A. Wittcoff, John


Wiley & Sons, New York, 1989.

3.

W.C. Foye, Principles of Medicinal Chemistry, Lea & Febiger, Philadelphia,


U.S.A.

Suggested
Readings
s:

1.

Strategies of Organic Drug Synthesis and Design, D. Lendnicer, John Wiley and


Sons, New York. 1998.


M.Sc PHARMACEUTICAL CHEMISTRY

(SEMESTER
-
I
V
)

PAPER
-
X
IV
:

DRUG DESIGN AND DRUG DEVELOPMENT
-
II

Time: 3 hours









Max Mar
ks: 75









Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Section A, B, C and D
will have two questions from the respective section
s of the syllabus and carry 12 marks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:

1.

Candidates are required to attempt one question
each from sections A, B, C and D


of the question paper and the entire section E.

2.

The use of scientific calculators is allowed.


SECTION
-
A

Role of Biotechnology in Drug Discovery

: Introduction,

, production of Human Proteins,

New ther
a
peuti
cs from Recombinant DNA technology , Protein engineering & Site
-
directed mut
a
genesis, Genetically engineered drug discovery tools
,
Natural Proteins,
as
leads for structurally m
odified proteins

: The Second Generation of Products from
Biotechnology, Examina
tion of the Structure and Function of Proteins as Tools for the
Evaluation of pathological processes: The Third Generation of Products from
Biotechnology.


S
ECTION
-
B


Designs of Enzyme inhibitor:


Mechanism of enzymatic catalysis. Transition state analog
s
as enzyme inhibitors. Kinetics of irreversible enzyme inhibition. Design of Reversible and
irreversible enzyme inhibitors with following examples: chymot
r
ypsin
, Subtilison,
Elastas
e
,

Pepsin
,
Cholinerterase, D
eaminases. Carboxypeptidase. G
lutamin syntheta
se .
Trisophosphate isomerase, Aldolase, Enolase, Decarboxylases, Lysozyme and other
glycosyl transferring enzymes. Creatine Kinase, adenylate Kinases. Asparatate
trancarbamolyase. Natural products as enzyme inhibitors. Penicillin, cephalosporin,
Le
upeptin
. Nojrimycin, Pentastati
n, Captopril, Sulphonamids.


SECTION
-
C

C
omputer Aided Drug Designing:
Computer requirement hardware, software
,

Data base
and information retrieval techniques. Graphical description of chemical structure.
Molecular interactions and
interactive
graphics. Introduction of molecular mechanics,
molecular
d
ynamics &
q
uantum mechanic
s (
semiempirical &
ab

init
io

methods
).
Mode
l
ling
in medicinal chemistry
-
uses and limitations. Logico structural approaches. Activity feature
selection within a g
roup of compounds, Activity profile selection.





SECTION
-
D

IPR:
Advantages of Patenting, Types of patents, brief introduction of patenting process.

Search for better and Safer Drugs:

Impact of External Factors
-
The Social, Financial,
and Working Environm
ent
:

Drug Therapy and Pub
l
ic opinion, Drug Research and
Financial Constraints, Working Climate for Innovative Drug Research.


Books Recommended:

1.

The Organic Chemistry of Drug Design and Drug Action, by R. B. Silverman,


Academic Press, 19
92.

2.

Drug Designs


A series of monographs in medicinal chemistry

edited by A.J.


Ariens. Ist edition, Vol. I, II, V, VIII & IX (only relevant chapters).

3.

Comprehensive medicinal chemistry. Peragmon Press. 1990, Vol. 4.

4.

Modern Drug Res
earch
,

Paths to Better and Safer Drugs, Medicinal research


series, volume 12, edited by Yvonne Connolly Martin, Eberhard Kutter, Vokhard


Austel.


Suggested
Readings
:

1.


Me
dicinal Chemistry for 21th century edited by C. G. Wermuth
, Blackwell


Scientific Publi
c
ations, 1997.































M.Sc PHARMACEUTICAL CHEMISTRY


(SEMESTER
-
I
V
)


PAPER
-
X
V
:
PHARMA
CEUTICAL

TECHNOLOGY
-
II

Time: 3 hours









Max Marks: 75










Lectures to be delivered: 60

INSTRUCTIONS FOR THE PAPER SETTERS:

The question paper will consist of five sections A, B, C, D and E. Section A, B, C and D
will have two questions from the respective sections of the syllabus and carry 12 ma
rks
each. Section E will consist of a short answer type question, which will cover the entire
syllabus uniformly and will carry 27 marks.

INSTRUCTIONS FOR THE CANDIDATES:

Candidates are required to attempt one question each from sections A, B, C and D of
the
question paper and the entire section E.


SECTION
-
A

Good manufacturing practices :
Current good manufacturing practices applied to
manufacturing, processing, packaging and holding of drugs.

ICH guidelines :
Need, for I CH norms, steps involved in I C
H process and introduction to
various guidelines . Discussion on I CH guidelines for testing stability of drug products.


SECTION
-
B

Sterilization Methods :

Introduction to various methods of sterilization
-

dry heat, moist
heat, gaseous and radiation.

Pa
renteral Dosage forms :

Pr
efor
mulation factors, concept of sterile

room

design and
maintenance, aseptic processing. Water for injection and its properties,
p
yrogen and
particulate matter testing, is
o
tonicity and its adjustment. Aque
ou
s and non
-
aqueous
ve
hicles for injectable preparations. Containers (glass and polyethylene) and closures for
in
je
ctable
s

and their evaluation.


SECTION
-
C

Modified Re
lease

Dosage Forms :

Basic characteristics of sustained, controlled, delayed
release oral dosage forms.
Factor
s influencing design and performance of oral MR dosage
forms.

Approaches used for design
ing

modified release oral dosage forms. Examples of
ingredients used and their characteristics. In vi
tro

a
nd

in vi
vo

evaluation

of drug release

and IVIC correlation.

N
ovel dr
ug

delivery systems
: Brief introduction with respect to advantages and
li
mitations of transdermal, vesicular (liposomes,
ni
osomes), osmotic pumps gastro
-
retentive dosage forms.


SECTION
-
D

Aerosols:

Advantages and limitations of
ae
ro
so
l drug delive
ry. Types of aerosol delivery
systems
.

Formulation ingredients, and evaluation of finished aerosols.





BOOKS RECOMMENDED

1.

S.H. Wiling, M. M., Tuckerman and W.S. Hitchings, Good Manufacturing Practice


for Pharmaceuticals, Marcel

Dekker Inc.,

New York, U.S.A., 1982.

2.

J.R. Robinson and V.H. Lee (eds.), Controlled Drug Delivery: Fundaments and


Application , 2
nd

edition, Marcel Dekker Inc., New
Y
ork, U.S.A. 1987.

3.

J.I. Wells. Pharmaceutical Preformulation: The physiological proper
ties of Drug



Substances, Ellis Horwood, Chicheater, U.K. 1987.

4.

Y.W. Chien (eds.), Novel Drug Delivery Systems, Marcel Dekker Inc., New York,


U.S.A., 1992.

5.

N.K. Jain (eds.), Controlled and Novel Drug Delivery, CBS Publishes and



Distributiors , New Delhi, India, 1997.








































M. Sc. PHARMACEUTICAL CHEMISTRY



(SEMESTER
-
I
V
)



Practical

Paper

VI
I
: Synthetic Medicinal Chemistry








Time: 4 hours


M. marks: 100





Total practical hours: 60





Suggested Experiments


Preparation/multistep synthesis, purifica
tion and spectroscopic characterization of organic
pharmaceuticals and intermediate given below: Acetanilide, Aspirin, Barbituric acid , Hippuric
acid, 3,4
-
dihydro
-
3
-
(P
-
methyl
-
1phenyl)
-
1
-
(2H)
-
Benzoxazine, Diketoperazine, Paracetamol,
thenacetin, Antipyrene
, 2
-
amino
-
5
-
bromopyridine, Nitrazepam, Azo sulfonamides,
sulfanilamide, Sulfathiazole, Diphenyhydantoin , Phenylbutazone, Nifedipine, Alcofenac,
Baclofen, Brimindiene, Tolmetin, procarbazine, Ketoprofen, Amphetamine,
Aminopyrine,tetrahydroisoquinolines.



Note
: Any other experiment (s) may be included in support of the theoretical aspect of course.