KUK - LMS

Syllabus

MODULE NO / UNIT	COURSE SYLLABUS CONTENTS OF MODULE	NOTES
Course Code: CHEM 305 Course Name: Pharmaceutical Chemistry Special-II
1	General mode of action, Medicinal Uses and Synthesis of Important Drugs in the Following Categories. Antineoplastic Agents: Metastasis, classification, mode of action of alkylating agents ( synthesis of mephalan, thiotepa, busulfan, lomustine) and antimetabolites ( synthesis of methotrexate, 5-fluorouracil, 6-mercaptopurine), hormone based therapies, plant products, radiotherapeutic agents. Taxol realated compounds. Antiviral agents: RNA and DNA viruses, An introduction to AIDS, how HIV infects the system, mode of action of nucleoside reverse transcriptase inhibitors- AZT, ddI, ddC, d4T & 3TC and HIV-protease inhibitors-Ritonavir. Synthesis of AZT. An overview of HIV entry inhibitors, Integrase inhibitors, Chemokine receptor binders, Inhibitors of gp41 fusion activity. Antimalarials: Cinchona alkaloids, 4-aminoquinolines, 8-aminoquinolines, Mefloquine, 9-aminoacridines. Synthesis of Mefloquine, chloroquine, primaquine.
2	Antibiotics Penicillins: Discovery, mode of action, SAR, Penicillins and semi-synthetic penicillins, problems of sensitivity to acids, bita-lactamases and narrow spectrum of activity; solving these problems leading to the development of penicillin V, oxacillin, cloxacillin, ampicillin, amoxycillin, carbenicillin and carfecillin; bita-lactamase inhibitors-Clavulanic acid, Olivanic acids. Cephalosporins: Classification, SAR, synthesis of cephalosporin-C, recent advances of fourth generation cephalosporins Sulfonamides-SAR, mode of action. Sulfanilamide analogs- synthesis of Sulfathiazole, sulfadiazine, sulfacetamide. Tetracyclins and aminoglycosides: Structure, mode of action, SAR, streptomycin, neomycin, gentamycin; Macrolides- mode of action, erythromycin, azithromycin; Synthesis of chloramphenicol. Quinolones, fluoroquinolones: Structure, mode of action, synthesis of nalidixic acid and ciprofloxacin Lincomycins.
3	Prostaglandins: General Introduction, nomenclature of prostaglandins and eicosanoid biosynthesis. Non-Steroidal anti-inflammatory agents: Classification, mode of action, COX-2 inhibitors, salol principle. Synthesis of celecoxib, valdecoxib, aspirin, phenbutazone, mefanamic acid, indomethacin, piroxicam, diclofenac, Naproxen. Antipyretic-Analgesics: opoid antagonists and agonists-codeine and heroin), synthesis of meperidine, methadone, dextropropoxyphen.
4	Antifertility agents: Ovulation inhibitors and related hormonal contraceptives- norethindrone, norethynodrel, estradiol and mestranol. Recent Advances. Antihypertensive agents: Classification, Hypertension, Renin-Angiotensin system, mode of action, Calcium channel blockers, ACE inhibitors and α-blockers, β-blockers, centrally acting adrenergic drugs, Synthesis of atenolol, clonidine, methyldopa, guanabenz, diltiazem, captopril, enalapril. Course outcome: The purpose of the paper to put forward the description of major classes of pharmaceutical agents especially the mode of action and synthesis.