Imperfect Pharmacy
B Pharmacy
Notes
6th Semester
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
OPEN UNIT 1
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.
OPEN UNIT 2
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.
OPEN UNIT 3
Unit 4
Antifungal agents:
Antifungal antibiotics: Amphotericin-B, Nystatin, Natamycin, Griseofulvin.
Synthetic Antifungal agents: Clotrimazole, Econazole, Butoconazole, Oxiconazole
Tioconazole, Miconazole*, Ketoconazole, Terconazole, Itraconazole, Fluconazole,
Naftifine hydrochloride, Tolnaftate.*
Anti-protozoal Agents: Metronidazole*, Tinidazole, Ornidazole, Diloxanide, Iodoquinol,
Pentamidine Isethionate, Atovaquone, Eflornithine.
Anthelmintic: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*, Albendazole,
Niclosamide, Oxamniquine, Praziquantel, Ivermectin.
Sulphonamides and Sulfones: Historical development, chemistry, classification and SAR
of Sulfonamides: Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*,
Sulphapyridine, Sulfamethoxazole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.
Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
Sulfones: Dapsone
OPEN UNIT 4
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, Hammett’s electronic parameter, Taft’s steric parameter and
Hansch analysis.
Pharmacophore modeling and docking techniques.
Combinatorial Chemistry: Concept and applications of combinatorial Chemistry: Solid phase and solution phase synthesis.