SVKM’s Narsee Monjee Institute of Management Studies

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Mumbai

School of Pharmacy & Technology Management, Shirpur
School of Pharmacy & Technology Management, Hyderabad
Program: B. Pharm Semester : VI
Course : Medicinal Chemistry III - Theory Code:BP601T
Teaching Scheme Evaluation Scheme
Lecture Term End
Practical Tutorial Internal Continuous
(Hours Examinations (TEE)
(Hours per (Hours Credit Assessment (ICA)
per (Marks- 75 in
week) per week) (Marks -25)
week) Question Paper)
3 NA 1 4 Marks Scaled to 25 Marks Scaled to 75
Prerequisite :
Basic knowledge of Organic Chemistry, Biochemistry, Physiology and Pharmacology.
Scope: This subject is designed to impart fundamental knowledge on the structure, chemistry
and therapeutic value of drugs. The subject emphasis on modern techniques of rational drug
design like quantitative structure activity relationship (QSAR), Prodrug concept, combinatorial
chemistry and Computer aided drug design (CADD). The subject also emphasizes on the
chemistry, mechanism of action, metabolism, adverse effects, Structure Activity Relationships
(SAR), therapeutic uses and synthesis of important drugs.
Objectives
Write the chemical synthesis of some drugs and to carry out synthesis of drug like molecules or
intermediates

Outcomes:
After completion of the course, students would be able to :
1. Explain and make use of the historical background, mechanism of action, Stereochemistry,
degradation and important products of antibiotics like beta lactam, tetracycline, macrolide,
aminoglycosides and miscelleneous
2. Compare and justify the use of medicinal agents based on the structure, classification, mode
of action, SAR, chemical synthesis and uses to treat malaria, tuberculosis and urinary tract
infections.
3. Compare and justify the use of medicinal agents from antifungal, anthelmentics, anti-viral
and sulphonamides class based on the structure, classification, mode of action, SAR, chemical
synthesis and uses thereof
4. Apply and propose the role of physiochemical parameters in drug design, prodrug, click and
combinatorial synthesis.
Detailed Syllabus: ( per session plan )

Unit Description Duration

in hours
Study of the development of the following classes of drugs, Classification, mechanism of
action, uses of drugs mentioned in the course, Structure activity relationship of selective class
of drugs as specified in the course and synthesis of drugs superscripted by (*)
1 Antibiotics 10
Historical background, Nomenclature, Stereochemistry, Structure activity
relationship, Chemical degradation classification and important products of
 SVKM’s Narsee Monjee Institute of Management Studies
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Mumbai
School of Pharmacy & Technology Management, Shirpur
School of Pharmacy & Technology Management, Hyderabad
the followingclassesalong with the drugs currently under clinical trials.
β-Lactam antibiotics: Penicillin, Cepholosporins, β- Lactamase inhibitors,
Monobactams, Carbapenems.
Aminoglycosides: Streptomycin, Neomycin, Kanamycin
Tetracyclines: Tetracycline,Oxytetracycline, Chlortetracycline,
Minocycline,Doxycycline
2 Antibiotics 10
Historical background, Nomenclature, Stereochemistry, Structure activity
relationship, Chemical degradation classification and important products of
the followingclassesalong with the drugs currently under clinical trials.
Macrolide: Erythromycin Clarithromycin, Azithromycin.
Glycopeptide, Polypeptide & lipopeptide antibiotics: Vancomycin, polymixin
B
Miscellaneous: Chloramphenicol*, Clindamycin, mupirocin and fusidic acid.
Antimicrobial resistance, causes and mechanism followed by intervention by
medicinal chemistry.
Antimalarials: Etiology of malaria.
Quinolines: SAR, Quinine sulphate, Chloroquine*, Amodiaquine,
Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride,Mefloquine.
Biguanides and dihydrotriazines: Cycloguanilpamoate, Proguanil.
Miscellaneous: Pyrimethamine, Artesunete, Artemether, Atovoquone
3 Anti-tubercular Agents 10
Synthetic anti tubercular agents: Isoniozid*, Ethionamide, Ethambutol,
Pyrazinamide, Para amino salicylic acid.*
Antitubercular antibiotics: Rifampicin, Rifabutin, Cycloserine,
Streptomycine, Capreomycinsulphate.
MDR and XDR TB and drugs: like Bedaquilline and Delamanidalong with
the drugs currently under clinical trials.
Urinary tract anti-infective agents
Quinolones: SAR of quinolones, NalidixicAcid,Norfloxacin, Enoxacin,
Ciprofloxacin*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin,
Moxifloxacin
Miscellaneous: Furazolidine, Nitrofurantoin*, Methanamine.
Antiviral agents:
Amantadine hydrochloride, Rimantadine hydrochloride,
Idoxuridinetrifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine,
Zalcitabine, Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir,
Indinavir, Ritonavir.
Neuraminidase inhibitor : Oseltamivir,
Drugs for the treatment of Ebola and SARS-Cov-2.
4 Antifungal agents: 8
Antifungal antibiotics: Amphotericin-B, Nystatin, Natamycin, Griseofulvin.
 SVKM’s Narsee Monjee Institute of Management Studies
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Mumbai
School of Pharmacy & Technology Management, Shirpur
School of Pharmacy & Technology Management, Hyderabad
Synthetic Antifungal agents: Clotrimazole, Econazole, Butoconazole,
OxiconazoleTioconozole, Miconazole*, Ketoconazole, Terconazole,
Itraconazole, Fluconazole, Naftifine hydrochloride, Tolnaftate*.
Anti-protozoal Agents: Metronidazole*, Tinidazole, Ornidazole, Diloxanide,
Iodoquinol, PentamidineIsethionate, Atovaquone, Eflornithine.
Anthelmintics: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*,
Albendazole, Niclosamide, Oxamniquine, Praziquantal, Ivermectin.
Sulphonamides and Sulfones
Historical development, chemistry, classification and SAR of Sulfonamides:
Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*,
Sulphapyridine, Sulfamethoxaole*, Sulphadiazine, Mefenide acetate,
Sulfasalazine.
Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
Sulfones: Dapsone*.
5 Introduction to Drug Design 7
Various approaches used in drug design.
Physicochemical parameters used in quantitative structure activity
relationship (QSAR) such as partition coefficient, Hammet’selectronic
parameter, Tafts steric parameter and Hansch analysis.
Introduction to QSAR
Exercises on identification of Drug receptor interactions from PDB using Co-
crystal structure of drugs and their molecular targets.
Pharmacophore modeling and docking techniques.
HTS, vHTS and Drug repurposing.
Combinatorial Chemistry: Concept and applications of combinatorial
chemistry: solid phase and solution phase synthesis.
6 Tutorials: Tutorial 15
1. Doubt clearing session and MCQs based test on unit 1, division is
Unit 2, Unit 3, Unit 4 and Unit 5. must in
2. Open Book assignments on critical problems at least 5. planning of
3. Class test (at least 2). course outline
4. Take home assignments, Involving the collection and for entire
presentation of Chemical scaffolds under development semester.
as drug with reference to syllabus which includes 1. 5 hrs.
a) Detailed SAR of drugs. 2. 5 hrs.
b) Mechanism of action at molecular level. 3. 2 hrs.
c) Review of synthetic methods for drugs 4. 3 hrs
d) New drugs entered in clinical trials.

Total 60
 SVKM’s Narsee Monjee Institute of Management Studies
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, Mumbai
School of Pharmacy & Technology Management, Shirpur
School of Pharmacy & Technology Management, Hyderabad
Text Books:
1. Organic and Pharmaceutical Chemistry by Wilson and Giswold, Wolters Kluwer India Pvt. Ltd.;
12th edition, 2010.
2. Principles of Medicinal Chemistry by Foye’s, Lippincott Williams and Wilkins; 7th, International
edition, 2012.
3. Text book of practical organic chemistry by A. I. Vogel, Pearson India, 3rd edition, 2010

Reference Books:
1. Burger's Medicinal Chemistry & Drug Discovery Abraham, D. J. Wiley–Blackwell; 6th
edition, 2007.
2. Textbook of Drug Design and Discovery by Larsen, P. K.; Liljefors, T.; Madsen, U. CRC
Press; 5th edition, 2016.
Any other information :
 en.wikipedia.org/wiki/Drug_design
 www.healthtech.com/2002/sbd/
 www.uic.edu/~kbruzik/text/phar331.htm
 www.answers.com/topic/drug-design
 publications.nigms.nih.gov/structlife/chapter4.html
 gtresearchnews.gatech.edu/newsrelease/cd4.htm

Total Marks of Internal Continuous Assessment (ICA) : 25 Marks

Distribution of ICA Marks :
Description of ICA Marks
Sessional Examination 15
Term Work 10
Total Marks : 25

____________ ____________
Signature Signature
(Prepared by) (Approved by)
Dr. Mayur Yergeri Dr. Bala Prabhakar
Dean, SPPSPTM