Medicinal Chemistry 3

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. 127 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. o