Welcome to the captivating realm of 6th semester Medicinal Chemistry 3! As we journey deeper into this subject, get ready to explore the intricate interplay between chemistry and pharmaceutical design. From dissecting complex molecular structures to unraveling the mechanisms behind drug interactions, this semester’s study material will illuminate the science that underpins life-changing medications. Let’s embark on this enlightening adventure together
Unit-1
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
Unit-2
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.
Unit-3
Anti-tubercular Agents
- Synthetic anti-tubercular agents: Isoniozid\*, Ethionamide, Ethambutol, Pyrazinamide, Para aminosalicylic acid.*
- Anti-tubercular antibiotics: Rifampicin, Rifabutin, Cycloserine Streptomycin, Capreomycin sulphate.
Urinary tract anti-infective agents
- Quinolones: SAR of quinolones, Nalidixic Acid,Norfloxacin, Enoxacin, Ciprofloxacin\*, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin, Moxifloxacin
- Miscellaneous: Furazolidone, Nitrofurantoin\*, Methenamine
Antiviral agents:
- Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine trifluoride, Acyclovir\*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine, Lamivudine, Loviride, Delavirding, Ribavirin, Saquinavir, Indinavir, Ritonavir.
Unit-4
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, Niclosanmide, 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*.
Unit-5
- 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 of combinatorial
- chemistry: solid phase and solution phase synthesis.
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