Medicinal Chemistry III - Theory

SVKM’s Narsee Monjee Institute of Management Studies
Pharmacy & Technology Management
Program: B. Pharm Semester : VI

Course : Medicinal Chemistry III - Theory Code:BP601T
Teaching Scheme Evaluation Scheme
Lecture Tutorial Term End
Practical Internal Continuous
(Hours (Hours Examinations (TEE)
(Hours per Credit Assessment (ICA)
per per (Marks- 75 in
week) (Marks -25)
week) 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:
Upon completion of the course student shall be able to
1. Understand the importance of drug design and different techniques of drug design.
2. Understand the chemistry of drugs with respect to their biological activity.
3. Know the metabolism, adverse effects and therapeutic value of drugs.
4. Know the importance of SAR of drugs.
Detailed Syllabus: ( per session plan )
Unit Description Duration
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 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.
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’selectronicparameter, 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 division is must
unit 1, Unit 2, Unit 3, Unit 4 and Unit 5. in planning of
2. Open Book assignments on critical problems at course outline
least 5. for entire
3. Class test (at least 2). semester.
4. Take home assignments, Involving the collection 1. 5 hrs.
and presentation of Chemical scaffolds under 2. 5 hrs.
development as drug with reference to 3. 2 hrs.
syllabus.which includes 4. 3 hrs
a) Detailed SAR of drugs.
b) Mechanism of action at molecular level.
c) Review of synthetic methods for drugs
d) New drugs entered in clinical trials.
Total 60
Text Books:
• Wilson and Giswold’s Organic medicinal and Pharmaceutical Chemistry.
• Foye’s Principles of Medicinal Chemistry.
• Burger’s Medicinal Chemistry, Vol I to IV.
• Introduction to principles of drug design- Smith and Williams.
• Remington’s Pharmaceutical Sciences
• Text book of practical organic chemistry- A.I.Vogel.
Reference Books:
• Abraham, D. J. Burger's Medicinal Chemistry & Drug Discovery 6th ed.; Wiley
Interscience: New Jersey, 2007.
• Hansch, C.; Sammes, P. G.; Taylor, J. B.; Kennewell, P. D. Comprehensive Medicinal
Chemistry, Vol 1, 1st ed.; Pergamon, 1989.
• Larsen, P. K.; Liljefors, T.; Madsen, U. Textbook of Drug Design and Discovery, 3rd ed.;
Taylor and Fransis: London and New York, 2004.
• Organic Chemistry by I.L. Finar, Vol. II.
• The Organic Chemistry of Drug Synthesis by Lednicer, Vol. 1-5.
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

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SVKM’s Narsee Monjee Institute of Management Studies

Pharmacy & Technology Management

Program: B. Pharm Semester : VI

Unit Description Duration

Study of the development of the following classes of drugs, Classification, mechanism of

Itraconazole, Fluconazole, Naftifine hydrochloride, Tolnaftate*.

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

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