B. pharma 6th Semester Medicinal Chemistry- III
UNIT- I
β-Lactam antibiotics: Penicillin, Cephalosporins, β- Lactamase inhibitors,
Monobactams
Aminoglycosides: Streptomycin, Neomycin, Kanamycin
Tetracyclines: Tetracycline, Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline
UNIT-II
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, Artesunate, Artemether, Atovoquone.
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, Methenamine.
Antiviral agents: Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine,
Lamivudine, Loviride, Delavirdine, Ribavirin, Saquinavir, Indinavir, Ritonavir.
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, Sulfamethoxazole, Sulphadiazine, Mafenide acetate, Sulfasalazine.
Folate reductase inhibitors: Trimethoprim, Cotrimoxazole.
Sulfones: Dapsone*
UNIT- IV
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