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MEDICINAL CHEMISTRY – III (Theory)


UNIT – I


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














UNIT – II



Antibiotics: Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation, classification and important products of the following classes.






Second material







UNIT – III


1. Anti-tubercular Agents




2. Urinary tract anti-infective agents






Miscellaneous: Furazolidine, Nitrofurantoin*, Methanamine.






3. Antiviral agents:


Second material




UNIT – IV


1. Antifungal agents:








Sulphonamides and Sulfones


Second material


Third material








UNIT – V



1. Introduction to Drug Design






Second material






Study of the development of the following classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted by (*)


UNIT – I

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, Clindamycin


Tetracyclines: Tetracycline,Oxytetracycline, Chlortetracycline, Minocycline, Doxycycline


UNIT – II

Antibiotics

Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degradation, classification and important products of the following classes.


Macrolide: Erythromycin, Clarithromycin, Azithromycin, Roxithromycin, Tilithromycin


Miscellaneous: Chloramphenicol*.


Prodrugs: Basic concepts and application of prodrug 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 – III

Anti-tubercular Agents


Synthetic anti tubercular agents: Isoniazid*, Ethionamide, Ethambutol, Pyrazinamide, Para aminosalicylic acid.*


Anti tubercular antibiotics: Rifampicin, Rifabutin, Cycloserine Streptomycin, Capreomycin sulphate.


Urinary tract anti-infective agents


Quinolones and fluoroquinolines: SAR of quinolones, Nalidixic Acid, Norfloxacin, Enoxacin, Ciprofloxacin*, Levofloxacin, Ofloxacin, Lomefloxacin, Sparfloxacin, Gatifloxacin, Moxifloxacin


Miscellaneous: Furazolidine, Nitrofurantoin*, Methanamine.


Antiviral agents: Amantadine hydrochloride, Rimantadine hydrochloride, Idoxuridine trifluoride, Acyclovir*, Gancyclovir, Zidovudine, Didanosine, Zalcitabine, Lamivudine, Loviride, Delavirdin, 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, Sulfamethoxaole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.


Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.


Sulfones: Dapsone*.


UNIT – V

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 of combinatorial chemistry: solid phase and solution phase synthesis.


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