Medicinal Chemistry 3 | B.Pharma 6th Semester Notes PDF

Syllabus
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.

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.