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Belec4sem4.doc

Elective Paper IV (Group B)
Medicinal Chemistry


I
Drug Design
Development of new drugs, procedures followed in drug design, concept of lead Compound and ead modification, concepts of prodrugs and soft drugs,structure-activity relationship (SAR) factors affecting bioactivity, resonance,inductive effect, isosterism, bio-isosterism, spatial,consideration. Therories of drugs activity; occupancy theory, rate theory,induced fit theory. Quantitative structure activity relationship.History and development of QSAR. Concepts of drugs receptors. Elementry treatment of drug receptors.Elementry treatment of drug receptor interactions. Physico-chemical parameters; lipophilicity, partion coefficient, electronic ionization constants, steric, Shelton surface activity parameter and redox potentials. Free-Wilson analysis, relationship between free-Wilson and Hansch analysis. LD-50, ED-50 (Mathematical derivations of equations excluded).
II Pharmacokinetis
Introduction to drug absorption , disposition, elimination using pharmacokinetics important pharmacokinetic parameters in defining drug disposition and in in therapeutics. Mention of uses of pharmacokinetics in drug development process
III Parmacodynamics

Introduction elementary treatment of enzyme stimulation, enzyme inhibition, sulphonamides, members active drugs, drug metabolism xenobiotics, biotransformation significance of drug medicinal chemistry.
IV Antineoplastic Agents
Introduction, cancer chemotheroy, special problemes, role of alkylating agents and antimetabolites in treatment of cancer.Mention of carcinolytic antibiotics and mitotic inhibitors. Synthesis of mechlorethamine, cyclophosphamide, melphalan, uracil, mustards, and 6-mercaptopurine.Recent development in cancer chemotherapy.Hormone and natural products. V Cardiovascular Drugs
Introduction, cardiovascular diseases, drug inhibitors of peripheral sympathic function, central intervention of cardiovascular output.Direct acting arteriolar dilators. Synthesis of amyl nitrate, sorbitrate, diltiazem, quinidine, verapamil, methyldopa, atenolol,oxyprenolol
VI Local Antiinfective Drugs 10 hrs
Introduction and general mode of action. Synthesis of sulphonamides,furrazolidone, nalidixin acid, ciproolloxacin, norfioxacin,dapsone, amino salicylic acid, isoniazid, ethionamide, ethambutal, fluconazole, econozole, griseofulvin, chkoroquin and primaquin. VII Psychoactive Drugs-The Chemotherapy of mind
Introduction ,neurotransmitters, CNS depressants, general anaesthetics, mode of action hypnotics, sedatives, anti-anxity drugs ,benzodiazepines, buspirone, neurochemistry of mental diseases.Antipsychotic drugs-the neuroleptics antidepressants, butyrophenones, serendipity and drugs development,stereochemical aspects of psychotropic drugs. Synthesisof diazepam, oxazepam, chloroazepum, alprazolam phenytoin, ethosuximde, trimethadione, barbiturates, thiopental sodium, guletehimide.
VII Antibiotics
Cell wall biosynthesis, inhiitors, -lactonem rings, antibiotics inhibiting protin synthesis.Synthesis of penicillin G, ampicillin, amoxicillin, chloramphenicol, cephalosporin, tetracycline and streptomycin.
Books Suggested:
1. Introduction to medicinal chemistry , Wiley-VCH
2. Wilson and Gisvold’s Text Book of organic Medicinal & Pharmaceutial Chemistry, Ed Robert F.
3. An Introduction to Drug Discovery,vol-1 (Chpter-9 and Ch-14), Ed.M.E.Wolff, John Wiley. 4. Burger’s Medicinal Chemistry & Drug Discovery,Vol-1(Chapter-9 & Ch-14),Ed.M.E.Wolff, John 5. Goodman and Gilman’s pharamacological Basis of Therapeutics, McGraw-Hill. 6. The Orgagnic Chemistry of Drug Design and Drug Action, R. B. Silverman, Academic Press. 7. Strategies for Organic Drug Synthesis and Design, D.Lednicer, John Wiely.

Source: http://lkouniv.ac.in/oldsite/chemistry/belec4sem4.pdf

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