M.

PHARMACY
PHARMACEUTICAL CHEMISTRY
I SEMESTER
Paper 101 - Modern Analytical Techniques
Paper 102 - Research Methodologies
Paper 103 - Advanced Pharmaceutical Organic Chemistry
Paper 104 - Advanced Chemistry of Natural Products
Paper 105 - Advanced Pharmaceutical Organic Chemistry - LAB
Paper 106 - Advanced Chemistry of Natural Products - LAB
Paper 107 - Seminar

II SEMESTER
Paper 201 - Advanced Medicinal Chemistry-I
Paper 202 - Advanced Medicinal Chemistry-II
Paper 203 - Bioassays & Pharmacological Screening Methods
Paper 204 - Drug Regulatory Affairs
Paper 205 - Advanced Medicinal Chemistry-I - LAB
Paper 206 - Advanced Medicinal Chemistry-II - LAB
Paper 207 - Seminar

III SEMESTER

Paper 301 - Project Seminar-I (On the proposed project work with aims and
objectives) - 50 Marks
Paper 302 - Project work - I

IV SEMESTER

Paper 401 - Project Seminar-II (On the experimentation and results of the
project work) – 50 Marks
Paper 402 - Project work - II
 SCHEME OF INSTRUCTIONS AND EVALUATION

PHARMACEUTICAL CHEMISTRY

FIRST SEMESTER

Evaluation / Marks

Paper Title of the Practical

Theory Total Credits
No. Paper
University University
Mid Mid
End End
Examination Examination
Examination Examination
Modern
Paper
Analytical 40 60 100 3
– 101
Techniques

Paper Research
40 60 100 3
– 102 Methodologies

Advanced
Paper Pharmaceutical
40 60 100 3
– 103 Organic
Chemistry
Advanced
Paper Chemistry of
40 60 100 3
– 104 Natural
Products
Advanced
Pharmaceutical
Paper
Organic 40 60 100 2
– 105
Chemistry
Practical

Advanced
Chemistry of
Paper
Natural 40 60 100 2
– 106
Products
Practical

Paper
Seminar 100 2
– 107

TOTAL 700 18
SECOND SEMESTER

Evaluation / Marks

Paper Title of the Practical

Theory Total Credits
No. Paper
University University
Mid Mid
End End
Examination Examination
Examination Examination
Advanced
Paper
Medicinal 40 60 100 3
– 201
Chemistry-I

Advanced
Paper
Medicinal 40 60 100 3
–202
Chemistry-II

Bioassays &
Paper Pharmacological
40 60 100 3
– 203 Screening
Methods
Drug
Paper
Regulatory 40 60 100 3
– 204
affairs
Advanced
Paper Medicinal
40 60 100 2
– 205 Chemistry-I
Practical
Advanced
Paper Medicinal
40 60 100 2
– 206 Chemistry-II
Practical
Paper
Seminar 100 2
– 207

TOTAL 700 18
THIRD AND FOURTH SEMESTERS

Credits
Paper No. III Semester Total
***

Project Seminar – I (On the proposed

Paper - 301 50 2
project work with aims and objectives)

Paper - 302 ---- 20

Project work - I
Total 50 22

Credits
Paper No. IV Semester Total
***

Project Seminar – II (On the Completed

Paper - 401 project work) 50 2

Project work - II
Paper - 402 --- 20

TOTAL MARKS
50 22

GRAND TOTAL FOR THE COURSE 1500 80

 SCHEME OF INSTRUCTION AND EVALUATION FOR
M. PHARM- PHARMACEUTICAL CHEMISTRY
I SEMESTER

PAPER 101: MODERN ANALYTICAL TECHNIQUES

(Paper Common for all Specializations)
Principles, instrumentation and applications of the following Instruments and
Chromatography techniques

Unit- I
i. UV- Visible spectrophotometry
ii. Infrared spectroscopy
iii. Spectrofluorimetry

Unit- II
i. NMR spectroscopy
ii. Electron Spin Resonance spectroscopy
iii. Atomic Emission spectroscopy

Unit- III
i. HPLC
ii. HPTLC
iii. Exclusion chromatography
iv. Super critical fluid chromatography

Unit- IV
i. Mass Spectroscopy including LCMS & GCMS
ii. GLC

Unit- V
i. Plasma Emission spectroscopy
ii. X-Ray diffractometry
iii. Optical Rotatory Diffusion
iv. Vapor phase chromatography
v. Affinity chromatography
vi. Ion-exchange chromatography
TEXT BOOKS
1. Practical Pharmaceutical Chemistry Vol. 1 &II by Beckett & Stenlake.
2. Instrumental Methods of Analysis by Scog and West.
3. Instrumental Methods of Analysis by B.K.Sharma
4. Vogel’s text book of Quantitative Chemical Analysis.
5. Instrumental methods of Analysis by Willard & Merrit.
6. A text book of Pharmaceutical Analysis by K. A. Conners.

REFERENCE BOOKS
1. I.P.
2. B.P.
3. U.S.P.
4. Remington’s Pharmaceutical Sciences.
5. Spectroscopy b Silversterin
 PAPER 102: RESEARCH METHODOLOGIES
(Paper common for all Specialization)

UNIT I
Statistical Methods:
Chance Variation – Probability Distribution - Normal Distribution – Sampling Distribution
Error and its significance-Measures of Error- Control of Error in Experimental Investigations
– Problem Solving.

UNIT II
Correlation and Regression, Multiple Regression - Problem Solving

UNIT III
Tests of Significance: Principles, t-test, z-test, F-ratio test, Chi-square test, Non-parametric
tests- their applications in pharmacy research with examples – Problem Solving

UNIT IV
Design of Experiments
Criteria of a good design with examples.
Principles- Randomization, replication and local control.
Study of CRD, RBD, LSD and factorial designs- their applications in Pharmacy research
with examples – Problem Solving

UNIT V
Analysis of Variance (ANOVA) – one way, two way and three way – principles and
applications in pharmacy research- Problem Solving
Optimization Techniques: Optimization Techniques based on Factorial Experiments -
Problem Solving.

Text & Reference Books:

1. Fundamentals of Biostatistics by Khan & Khanum, 3rd Revised Edition, Ukaaz
Publications, Hyderabad
2. Theory & Practice of Industrial Pharmacy by Leon Lachman and Others
3. Remington’s Practice of Pharmaceutical sciences, (Latest Edition)
4. Principles of Biostatistics by Marcello Pagnano, Published by Brooks/Cole, (Saurabh
Printers Pvt. Ltd)
 PAPER 103: ADVANCED PHARMACEUTICAL ORGANIC CHEMISTRY

Unit-I
Stereochemistry:
Elements of symmetry, Plane of symmetry, Centre of symmetry, Alternative axis of
symmetry, Simple axis of symmetry, kinds of molecules displaying optical activity.
Notation, Relative configuration and Absolute configuration .Compounds with a chiral
carbon atom, compounds with other Quadrivalent chiral atoms. Optical isomerism in
compounds containing no chiral atom, biphenyl, allenes, compounds with exocylic
double bonds and spirans. Chirality due to helical shape, chirality caused due to restricted
rotation (other types).
Cis / Trans, E – Z isomerism resulting from double bonds, monocyclic compounds, fused
ring system. Racemic modifications and methods for resolution of racemic mixtures.
Asymmetric synthesis and stereo – selective synthesis.

Unit-II
Reactive Intermediates:Definitions, Generation, stability, Structure and Reactivity of free
radicals, carbocations, carbanions, carbenes, Nitrenes/Nitrenium ions.
Mechanisms of organic reactions: Free radicals (addition and substitution), Electrophilic
(addition and substitution). Nucleophilic (addition and substitution).
Concepts of Aromaticity involving ring systems,. Aromatic Substitution reactions,
Electrohilic aromatic substitution. Mechanisms, Orientation and Reactivity.

Unit-III
Elimination Reactions: E2, E1CB and E2C mechanisms, Mechanisms and orientation in
Pyrolytic eliminations, effect of substrate structure, Attacking base, leaving group and
reaction bond,medium and reactivity addition to carbon – carbon multiple bond
reactions. Mechanisms,Orientation and reactivity.
Electrocyclic, pericyclic and sigmotropic reactions: introduction, terminology and
mechanism with suitable examples.

Unit-IV
Molecular Rearrangements & their applications:
Carbon to Carbon Migration: Wagner – Meerwin rearrangement, Claisen rearrangement
and Benzil – Benzilic acid rearrangement.
Carbon to Nitrogen Migration: Hoffmann rearrangement, Curtius rearrangement and
Lossen rearrangement, Beckman rearrangement.
Carbon to Oxygen Migration: Bayer – Villiger rearrangement, Rearrangement of hydro
peroxides and Wittig rearrangement.
Synthetic Reagents & Applications: Lead Tetra Acetate (LTA), N- Bromosuccinimide
(NBS), Osmium Tetroxide, Lithium Aluminum Hydroxide and Sodium Bromohydride.
Unit-V
Unit Process in Organic Synthesis: Catalytic hydrogenation, Nitration, Sulphonation,
Halogenation, Amination, Acetylation, Esterification and Hydrolysis
Scale Up Techniques for process optimization, Maximization of productivity,
in – process control techniques with examples. Chemical Technology of selected bulk
drugs – Ibuprofen, Paracetamol, Ciprofloxacin and Isosorbide Nitrate.
Synthetic Strategies: Introduction, Target selection , Retro synthesis , various strategic
approaches, criteria or a disconnection of strategic bonds, strategic bonds in rings,
Dégradation techniques for retro synthesis.

Recommended Books:

1. Francis A. Carey & Richard J. Sunberg, Advanced Org. Chemistry , III rd Edition , Par
B; Reactions and synthesis , Plenum Press, new York , London , Latest Edition.
2. Eliel I. Ernest and Samuel h, Stereochemistry of Org. Compounds, John Wiley and sons,
New York, 2003 Edition.
3. Roland E. Lehr & Alan P Marchard, Orbital Symmetry: A Problem solving approach,
Academic Press, New York Latest Edition.
4. J. March , Advanced Org. Chemistry , Reactions Mechanisms and Structure , 4th Edition,
John Wiley & Sons , New York Latest Edition
5. I. L. Finar , Organic Chemistry , ELBS
6. Herbert O. Modern Synthesis Reactions IInd Edition W.A. Beenamis Inc. Menco Park
California
7. W. Carruthers , Some Modern Methods of Org. Synthesis , III rd Edition , Cambridge
University Press, Cambridge(1988)
8. Groggins, Unit process in Org. Synthesis, McGraw Hill Book Crop.
9. S. Warren, Org. Synthesis. The Disconnection Approach, J. Wiley & Sons. NY
10. Gorgy Keri and Istarian Toth , Molecular Patho-mechanisms and New Trends in Drug
Research – Taylor and Francis Group ,London 2003
11. R.K. Mackie , A Guidebook to Organic Thesis – Prentice Hall
12. T.W. Greene and PGM Warts ,Protecting Groups – John Willey
13. Michael B. Smith , Organic Synthesis
 PAPER 104: ADVANCED CHEMISTRY OF NATURAL PRODUCTS

Unit-I
General Methods of Extraction, Qualitative chemical test for the detection of various natural
product compounds. Study of herbal extracts – processing, equipment and analytical profile
of extracts of drugs.
Isolation/Separation techniques –The technique and application of thin layer chromatography
and Preparative TLC, Column chromatography – medium and high-pressure liquid column
chromatography, Flash chromatography, HPTLC, HPLC and GC – normal and reverse phase
techniques.

Unit-II
Alkaloids - Introduction, general methods of structure elucidation, chemistry and structure
elucidation of Morphine, Reserpine and Quinine. Isolation procedure of Piperine and
Quinine.

Unit-III
Steroids – Introduction, nomenclature and stereochemistry of different steroidal skeletons.
Chemistry of cardiac glycosides, progesterone, oestradiol, cortisone, testosterone, bile acids.
Chemistry and structural elucidation of cholesterol.. Synthesis of stilbesterol & hexesterol,
Isolation procedures for diosgenin and sennosides.

Unit-IV
Polypeptides and Proteins – Introduction and general methods of separation, general methods
of degradation and end group analysis, general methods of synthesis of peptides, Sequence
analysis, secondary and tertiary structure of proteins, chemistry of insulin.

Unit-V
Natural Products as Leads for New Drugs:
Introduction, History, approaches to discovery and development of natural products as
potential new drugs, selection and optimization of lead compounds for further developments
from CNS, Anticancer, Antibiotic and Cardiovascular drugs.

Recommended Books:
1. Organic Chemistry Vol. 2nd by I. L. Finar
2. Org. Chemistry by Morrison & Boyd
3. Alkaloids – Chemical & Biological Prospective by S. W. Pelletier
4. Steroids by Fischer and Fischer
5. Pharmacognosy by Trease & Evans
6. Chemistry of Natural Products – Ata Ur Rehman
7. Natural Products – A Lab Guide by Raphael Ikon
Paper 105 - Advanced Pharmaceutical Organic Chemistry LAB
(Based on Theory at least 10 Experiments)

Paper 106 - Advanced Chemistry of Natural Products LAB

(Based on Theory at least 10 Experiments)
 IInd SEMESTER
Paper 201: ADVANCED MEDICINAL CHEMISTRY – I

Unit-I
Theoretical Aspects of Drug Action:
Types of drug action, physicochemical parameters and pharmacological activity,
Non empirical Electronic parameters, steric parameters and Stereo Chemical
aspects of Drugs. Drug Receptors, Receptor types and isolation, Drug Receptor
Interaction, theories of drug action, mechanism of drug action.

Unit-II
Targets for the development of following chemotherapeutic agents:
Anti-tubercular, Anti- HIV, anticancer, anti – fungal, Immuno- modulators,
anti- amoebic drugs.
Targets for the development of following pharmacodynamic agents:
Anti-ulcer, Analgesic, Anti Inflammatory, Anti atherosclerotic, Anti- angiogenesis,
Anti – hypertensives.

Unit-III
Biotransformation of drugs:
Prodrug approach, Soft Drug approach, enzymes responsible for biotransformation,
microsomal and non microsomal mechanisms. Factors influencing enzyme induction
and inhibition.

Unit-IV
Design of Local anesthetics:
Introduction, general considerations on the development of new drugs, classical and
rational procedures for the development of local anesthetics
Unit-V
Antipsychotic Agents:
Role of Dopamine, Serotonin, Glutamate and their receptors. SAR and
Pharmacokinetics of Ticyclic Neuroleptics, Butyrophenones and Benzamides.
A brief account of non – benzodiazepine agonist.

Recommended Books:
1. Richard B. Silvermann, Org. Chemistry of Drug Design and drug Action.
2. Berger’s Medicinal Chemistry and Drug Design. 6th Edition.
3. Korolkovas Essentials of Medicinal Chemistry
4. Purcell Strategies of Drug Design
5. Alfred Berger Biochemical Basis of Drug Design
6. Corwin , Hansen Comprehensive Medicinal Chemistry
7. William O Foye Medicinal Chemistry
8. Testa B and Jenner P. Drug Metabolism Chemical & Biochemical Aspects, Marcel
Dekker
9. Gyorgy Keri & Istdan Toth Molecular Pathomechanism and New Trends in Drug
Research, Taylor & Francis Pub.
10. Ariens. Drug design medicinal chemistry a series of monograph-volume 11- III,
academic press, an imprint of Elsevier pub.
Paper 202: ADVANCED MEDICINAL CHEMISTRY – II

Unit-I
Genesis of New Drugs: Serendipity, Random Screening, Extraction of active principles from
Natural Sources, Molecular Modification of Known Drugs, Selection or Synthesis of Soft
Drugs, Drug Latentiation and rational drug design

Unit-II
Rational Drug Design: QSAR: Parameters involved in QSAR, lipophilicity (Polarisabiltiy,
electronic and steric parameters). Quantitative models. Hansch Analysis, Free Wilson
Analysis and their relationships, linear relationships and applications of Hansch and Free
Wilson Analysis.

Unit-III
Molecular Modeling: Introduction, molecular methods, Known receptors, unknown
receptors.

Unit-IV
Enzyme Inhibitors: A detailed study of the following types of enzyme inhibitors ,related
drugs and their pharmaceutical significance :
a. P.G. Synthetase (Cycloxygenase & Lipoxygenase Inhibitors)
b. Phosphodiesterase (PDE ) Inhibitors
c. Carbonic Anhydrase Inhibitors.
d. Angiotensin Converting Enzyme (ACE) Inhibitors
e. Acetyl Cholinesterase (Ach E) Inhibitors.

Unit-V
Combinatorial Chemistry – Parallel Synthesis, real combinatorial chemistry and
deconvolution methods.

Recommended Books:
1. Berger’s Medicinal Chemistry and Drug Design. 6th Edition
2. Korolkovas Essentials of Medicinal Chemistry
3. William O Foye Medicinal Chemistry
4. Lednicer, Organic Chemistry of Drug Synthesis
5. Ariens ,Drug Design , Academic Press
6. Purcell Strategies of Drug Design
7. Corwin , Hansen Comprehensive Medicinal Chemistry
8. Richard B. Silvermann, Org. Chemistry of Drug Design and drug Action
9. Smith and Williams , Introduction to principles of Drug Design – Harwood Academy
Press.
10. Gyorgy Keri & Istdan Toth Molecular Pathomechanism and New Trends in Drug
Research, Taylor & Francis Pub
11. Thomas Nogrady, Medicinal Chemistry. A biochemical Approach, Oxford Univ. Press.

Paper 203: BIOASSAYS & PHARMACOLOGICAL SCREENING METHODS

Unit I:
Principles of Experimental Pharmacology and Drug Discovery:
Common laboratory animals in Pharmacological research, Limitations of animal tests,
Alternatives to animal use, Anesthetics used in laboratory animals, some standard
techniques used in handling laboratory animals, Euthanasia of experimental animals.
Regulation for the care and use of laboratory animals.
Strategies and approaches employed in drug discovery. Basic concepts of Combinatorial
chemistry, High throughput screening, Cell lines and their applications in drug discovery.
Transgenic animal models in the development of new drugs.

Unit II:
Principles of Biological standardization: Statistical treatment of modern problems in the
biological evaluation of drugs. Methods used in the bio-assays for antibiotics and
microbiological assays. Bioassay for Diphtheria antitoxin; Tetanus; Cholera vaccine;
Posterior Pituitary extract; Adrenaline; Heparin; Digitalis; d-Tubocurarine; Vitamins.
Test for pyrogens.
Bioassay methods for autocoids – Development of new bio-assay methods. Assays using
special designs for experiments to eliminate known source of variation. Toxicity tests,
Determination of LD50, Acute, Sub acute, and Chronic toxicity studies – Tests for
freedom from undue toxicity of drugs.

Unit III:
Basic Principles of Screening and types – Simple, Blind and Programmed Screening. Need
for isolated tissues in pharmacological evaluation of drugs.
Organization of screening for the Pharmacological activity and evaluation of new
substances in CVS:
1. Diuretics
2. Antihypertensives
3. Antianginal agents
4. Anti arrhythmic agents and agents used in sudden cardiac failure
5. Druigs used in cardiomyopathies
6. Drugs used in hyperlipidemia and atherosclerosis
7. Anti infarct agents

Unit IV:
Organization of screening for the Pharmacological activity and evaluation of new substances
in CNS:
1. Anti-epileptics
2. Anti-anxiety agents and Drugs used in mood and sleep disorders
3. Antipsychotics
 4. Drugs affecting memory
5. Drugs used in Alzheimer’s disease
6. Local Anesthetics
7. Skeletal muscle relaxants and Neuromuscular blockers

Unit V:
Organization of screening for the Pharmacological activity and evaluation of new substances
1. Anti-diabetic agents
2. Analgesics and Drugs used in arthritis and neuropathic pain
3. Anti-Inflammatory agents
4. Anti-asthmatic agents
5. Anti-ulcer agents
6. Hepatoprotective agents

Recommended Books:
1. H.G.Vogel (ed),Drug Discovery and Evaluation- Pharmacological Assays, 2nd Edition,
Springer verlag,Berlin,Germany,2002.
2. M.N.Gosh, Fundamentals of Experimental pharmacology, 2nd Edition, Scientific Book
Agency,Culcutta,India,1985.
3. D.R.Laurence and A.L.Bacharach (Eds), Evaluation of Drug Activities:
Pharmacometrics, Volume I and II, Academic press, London,U.K,1964.
4. Biological Standardization by J.H.Burn, D.J.Finney and L.G. Goodwin.
5. Pharmacopoeias: IP,BP,USP
6. Screening methods in pharmacology by Robert A.Turner.
7. Methods in Pharmacology by Swarbrick.
 Paper 204: DRUG REGULATORY AFFAIRS:
(Paper Common for all Specializations)

Unit – I
Formulation development: Regulatory requirements involved in the preformulation
studies, solid, liquid and semi-solid dosage forms, controlled release preparations,
injections, ocular preparations as per the European community, United States and Indian
regulatory authorities

Unit - II
Manufacturing: Regulatory requirements as per European community, United States and
Indian regulatory authorities for manufacturing information, manufacturing formula,
process, validation of manufacturing process, equipment, documentation, inspection
requirement of regulatory guidelines for active ingredients, data requirement for new
drug, International aspects of Excipients, approval as per guidelines of all the territories.
Regulatory guidelines for packaging materials, test and evaluation of packaging
materials, biological test, elastometer test, microbiological test and evaluation of closures.

Unit - III
Stability testing: Scientific and technical background to the design of stability testing
regulatory requirements as per European community, United States and Indian regulatory
authorities for testing of new active substances, bulk active drug substances, dosage form
in their final packaging. Extension of shelf-life after authorization of drug international
harmonization and current guidelines. Regulatory affairs in respect of residual solvents as
per the ICH guidelines, analytical method validation, pharmacokinetic and toxicokinetic
validation.
Biopharmaceutics: Different testing parameters and standards as per regulatory
requirements of European community, United States and Indian regulatory authorities
with respect to factors related to formulation, dosage form, manufacturing process,
stability and storage.

Unit - IV
Preclinical aspects of Biopharmaceutics: Current guidelines and developments as per
regulatory requirements of European community, United States and Indian regulatory
authorities in respect of clinical bioavailability , study design, presentation documentation
and statistical analysis
Clinical pharmacology and Pharmacodynamics: Regulatory guidelines as per European
community, United States and Indian regulatory authorities on clinical study design,
documentation, presentation and interpretation. Clinical trials: Definition, phase I, phase
II, phase III and phase IV studies, design documentation, presentation and interpretation,
statistical analysis of clinical data and factorial design.
Unit - V
Intellectual property rights and patents: Introduction, purpose, international scenario and
Indian scenario, guidelines as per European community, United States and Indian
regulatory authorities, documentation, presentation and application, procedure for
obtaining and writing a patent and patenting rules and regulations

References:
1. Quality Assurance Guide by Organization of Pharmaceutical producers of India.
2. Drug formulation manual by D.P.S. Kohli and D.H.Shah. Eastern publishers, New Delhi.
3. How to practice GMPs by P.P.Sharma. Vandhana Publications, Agra.
4. Pharmaceutical Process Validation by Fra. R. Berry and Robert A. Nash.
5. Pharmaceutical Preformulations by J.J. Wells.
6. Applied production and operations management by Evans, Anderson, Sweeney and
Williams.
7. Basic Principles of Clinical Research and Methodology by Gupta.
8. Biopharmaceutics and Clinical Pharmacokinetics-An introduction; 4th edition, Revised
and expanded by Robert. E. Notari, Marcel Dekker Inc, New York and Basel, 1987
Paper 205: Advanced Medicinal Chemistry-I Practical

BASED ON THEORY AT LEAST 10 EXPERIMENTS

Paper 206: Advanced Medicinal Chemistry-II Practical

BASED ON THEORY AT LEAST 10 EXPERIMENTS