Syllabus
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Course Code: CHEM 404 Course Name: Organic Chemistry Special-VI |
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| MODULE NO / UNIT | COURSE SYLLABUS CONTENTS OF MODULE | NOTES |
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| 1 | Drug Design Classification and discovery of new drugs, history and development of chemotherapeutic agents, therapeutic index, LD50 and ED50, naming of (new) drugs. Elementary idea about drug action: the receptor role, neurotransmitters and receptors, ion channels and their control. Membrane bound enzymes-activation/deactivation. Chemical basis of messenger induced change of shape by the receptor. Design of agonists, antagonists and partial agonists. Drug development: Screening of natural products, isolation and purification, structure determination, structure-activity relationships (SAR), synthetic analogues, isosteres and bioisosteres, concept of lead compounds. Brief overview of pharmacokinetics and pharmacodynamics, concept of prodrug and synergism. |
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| 2 | Synthesis, General Mode of Action and Medicinal Uses of Important Drugs in the Following Categories. Antineoplastic Agents: Mechlorethamine, Chlorambucil, cyclophosphamide, carmustine, aminopterin, 6-mercaptopurine, paclitaxel (synthesis of paclitaxel excluded). Antimalarials: Chloroquine, primaquine, chloroguanide, pyrimethamine. Analgesics, Antipyretics and Antiinflammatory agents: Morphine and related compounds (codeine and heroin), meperidine, methadone, aspirin, acetaminophen, indomethacin, phenylbutazone, mefenamic acid, ibuprofen, diclofenac, naproxen, celecoxib. Antifertility agents: Ovulation inhibitors and related hormonal contraceptives - norethindrone, norethynodrel, estradiol, mestranol, non hormonal contraceptive- centchroman (synthesis of all the drugs excluded). Cardiovascular Drugs: Calcium channel blockers and β-blockers: sorbitrate, diltiazem, atenolol and verapamil. AIDS and drugs against HIV: HIV infection to the system, structure and mode of action of important drugs against HIV (nucleoside reverse transcriptase inhibitors) - AZT, ddI, ddC, d4T and 3TC (synthesis only of AZT). |
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| 3 | Antibiotics Cell wall biosynthesis and protein synthesis inhibitors: Penicillins and semi-synthetic penicillins. synthesis, structure elucidation and medicinal uses of penicillin G, problems of sensitivity to acids, β-lactamases and narrow spectrum of activity, solving these problems leading to the development of penicillin V, oxacillin, cloxacillin, ampicillin, amoxicillin, carbenicillin and carfecillin. Cephalosporins - Discovery, structure elucidation and synthesis of cephalosporin-C. |
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| 4 | Alkaloids Definition, nomenclature and physiological action, occurrence, isolation, general methods of structure elucidation, degradation, classification based on nitrogen heterocyclic ring, role of alkaloids in plants. Structure, stereochemistry, synthesis and biosynthesis of the following: Ephedrine, (+)-Coniine, Nicotine, Quinine and Reserpine. |
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