COURSE SUMMARY
Course Title: 
Medicinal Chemistry III – Theory
Course Code: 
BP505T
Year Taught: 
2014
2015
2016
2017
2018
Semester: 
5
Degree: 
Undergraduate (UG)
School: 
School of Pharmacy
Campus: 
Kochi

'Medicinal Chemistry III – Theory' is a course offered in the sixth semester of B. Pharm program at School of Pharmacy, Health Sciences campus, Amrita Vishwa Vidyapeetham.

Course Duration: 45 Hours

Scope:

This subject is designed to impart fundamental knowledge on the structure, chemistry and thera- peutic value of drugs. The subject emphasis on modern techniques of rational drug design like quantitative structure activity relationship (QSAR), Prodrug concept, combinatorial chemistry and Computer aided drug design (CADD). The subject also emphasizes on the chemistry, mechanism of action, metabolism, adverse effects, Structure Activity Relationships (SAR), therapeutic uses and synthesis of important drugs.

Objectives:

Upon completion of the course student shall be able to

  1. Understand the importance of drug design and different techniques of drug design.
  2. Understand the chemistry of drugs with respect to their biological activity.
  3. Know the metabolism, adverse effects and therapeutic value of drugs.
  4. Know the importance of SAR of drugs.

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 (10 Hours)

Antibiotics: Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degrada- tion 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 II (10 Hours)

Antibiotics: Historical background, Nomenclature, Stereochemistry, Structure activity relationship, Chemical degrada- tion 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 (10 Hours)

Anti-tubercular Agents

Synthetic anti tubercular agents: Isoniozid*, Ethionamide, Ethambutol, Pyrazinamide, Para amino sali- cylic 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, Lome- floxacin, 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 IV (08 Hours)

Antifungal agents:

Antifungal antibiotics: Amphotericin-B, Nystatin, Natamycin, Griseofulvin.

Synthetic Antifungal agents: Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole, Mi- conazole*, 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, Sulfisoxaz- ole, Sulphamethizine, Sulfacetamide*, Sulphapyridine, Sulfamethoxaole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.

Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.

Sulfones: Dapsone*.

Unit V (07 Hours)

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.