BP601T. MEDICINAL CHEMISTRY – III Books
“Medicinal Chemistry III: Advanced drug design and synthesis, including SAR, molecular modeling, and lead optimization.”
Course Content
Unit Title
Content
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
- Tetracyclines: Tetracycline, Oxytetracycline,
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.
- 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-III
- 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, 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-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, Sulphapyridine, Sulphamethizine, Sulfacetamide*, 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
chemistry: solid phase and solution phase synthesis.
Learning Objectives
- Understand the importance of drug design and different techniques of drug design.
- Understand the chemistry of drugs with respect to their biological activity
- Know the metabolism, adverse effects and therapeutic value of drugs.
Share on WhatsApp