B.Pharm Medicinal Chemistry 3 Notes

MEDICINAL CHEMISTRY 3 UNIT-WISE NOTES – BP601T

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 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.

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, 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*.

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
• chemistry: solid phase and solution phase synthesis.