Medicinal Chemistry III Book B.Pharm 6th Semester

Syllabus

Module 01                                                                                       10 Hours

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.

Module 02                                                                                       10 Hours

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.

Pro-drugs

• 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.

Module 03                                                                                       10 Hours

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.

Module 04                                                                                       08 Hours

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.

Module 05                                                                                       07 Hours

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.