Syllabus Medicinal Chemistry - III UNIT - I • Antibiotics : Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation classification and important products of the following classes. • β-Lactam antibiotics : Penicillin, Cepholosporins, β- Lactamase inhibitors, Monobactams • Aminoglycosides : Streptomycin, Neomycin, Kanamycin • Tetracyclines : Tetracycline, Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline. (Chapter 1) UNIT - II • Antibiotics : Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation classification and important products of the following classes. • Macrolide : Erythromycin Clarithromycin, Azithromycin. • Miscellaneous : Chloramphenicol*, Clindamycin. • Prodrugs : Basic concepts and application of prodrugs design. • Antimalarials : Etiology of malaria. • Quinolines : SAR, Quinine sulphate, Chloroquine*, Amodiaquine, Primaquine phosphate, Pamaquine*, Quinacrine hydrochloride, Mefloquine. • Biguanides and dihydro triazines : Cycloguanil pamoate, Proguanil. • Miscellaneous : Pyrimethamine, Artesunete, Artemether, Atovoquone. (Chapter 2) UNIT - III • Anti-tubercular Agents • Synthetic anti tubercular agents : Isoniozid*, Ethionamide, Ethambutol, Pyrazinamide, Para amino salicylic acid.* • Anti tubercular antibiotics : Rifampicin, Rifabutin, Cycloserine Streptomycine, Capreomycin sulphate. • Urinary tract anti-infective agents • Quinolones : SAR of quinolones, Nalidixic Acid,Norfloxacin, Enoxacin, Ciprofloxacin*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin, Moxifloxacin • Miscellaneous : Furazolidine, Nitrofurantoin*, Methanamine. • Antiviral agents : Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine, Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir, Indinavir, Ritonavir. (Chapter 3) UNIT - IV • Antifungal agents : • Antifungal antibiotics : Amphotericin-B, Nystatin, Natamycin, Griseofulvin. • Synthetic Antifungal agents : Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole, Miconazole*, Ketoconazole, Terconazole, Itraconazole, Fluconazole, Naftifine hydrochloride, Tolnaftate*. • Anti-protozoal Agents : Metronidazole*, Tinidazole, Ornidazole, Diloxanide, Iodoquinol, Pentamidine Isethionate, 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*. (Chapter 4) UNIT - V • Introduction to Drug Design : Various approaches used in drug design. • Physicochemical parameters used in quantitative structure activity relationship (QSAR) such as partition coefficient, Hammet’s electronic parameter, Tafts steric parameter and Hansch analysis. • Pharmacophore modeling and docking techniques. • Combinatorial Chemistry : Concept and applications chemistry : Solid phase and solution phase synthesis. (Chapter 5)
