JAWAHARLAL NEHRU TECHNOLOGICAL UNIVERSITY HYDERABAD

Course Objectives

The drug discovery and design with respect to the lead molecules and its

optimization is clearly discussed. The concept of CADD is also discussed. Sufficient information about various antibiotics and their chemotherapeutic agents are also studied in depth.

Course Outcome

The students would be in a position to participate in the community pharmacy

activities with the knowledge they gained through the study of the various topics of the syllabus.

UNIT - I

• (a) Drug discovery and drug design. Introduction to discovery of lead molecule, lead optimization, pharmacophore identification, General structure activity relationship studies,
• (b) Computer aided drug design: Introduction to CADD, Parameters in QSAR, Hansch analysis, Free Wilson analysis

UNIT - II

• a. Antibiotics: Brief historical background, definition, classification of antibiotics. Penicillins: Historical background and biological sources. Structures of different penicillins. Reactions: Hydrolysis of penicillin by cold and hot dilute mineral acid, alkali, enzymatic hydrolysis with Pencillinase, amidase. Classification: Oral and parenteral, based on spectrum of β, γ – lactamase, as natural, biosynthetic and semi-synthetic. General method of synthesis of pencillins from 6-APA, SAR, mechanism of action, therapeutic uses, toxicity. β –lactamase inhibitors.
• b. Cephalosporins: Structures of some important compounds (Cephalosporins, Cephamycins. Cefadroxil, Cefoxitin. Acid hydrolysis of Cephalosporin C. Comparison of 6-APA and 7-ACA, penam and cepham. Classification: Generations of cephalosporins, Oral and parenteral, SAR and Advantages over penicillins.

UNIT - III

a.Tetracyclins: Biological sources, structures of the important tetracyclines, important structural units and the three acidity constants in the tetracycline molecule, Amphoteric nature, mechanism of action, spectrum of activity, SAR and toxicity.

• b. Aminoglycosides: Structure of streptomycin, acid hydrolysis, mechanism of action, therapeutic uses and toxicity. Dihydrostreptomycin and its importance and mention other aminoglycoside antibiotics. A brief account of chloramphenicol and its synthesis, macrolide and polypeptide antibiotics and rifampicin (Structures not included).
• c. Quinoline type: Ciprofloxacin & norfloxacin

UNIT - IV

Chemotherapeutic Agents:

• a. Sulphadrugs : Sulphadiazine, Suphasalzine Trimethoprim, Sulphamethoxazole, Sulphameter
• b. Antifungal Agents : Fluconazole and Itraconazole.
• c. Anti viral Drugs : Acyclovir, Zidovudine
• d. Anti tubercular agents : Isonicotinic acid hydrazide and ethambutol R16 B.PHARMACY IV YEAR
• e. Anti leprotic agents : Dapsone, clofazemine
• f. Antiamoebics : Metronidazole, diloxanide furoate
• g. Anthelmintics : Diethylcarbamazine citrate, pyrante pamoate, mebendazole, lbendazole
• h. Antimalarial drugs : Chloroquine, primaquine and pyrimethamine, norflaxacin and ciprofloxacin

UNIT - V

• a. Anticancer Drugs: Chlorambucil, busulphan, procarbazine, carmustine, 5-flurouracil, 5- mercaptopurine methotrexate, vinca alkaloids – vinblastin, vincristine
• b. Immunosuppressive agents. Brief introduction to therapeutic agents developed from recombinant DNA technology
• c. Diagnostic agents and radioprotective agents.

TEXT BOOKS

• 1. William O. Foye, Textbook of Medicinal Chemistry, Lea & Febiger, Philadelphia.
• 2. JH Block & JM Beale, Wilson & Giswold’s Text book of organic Medicinal Chemistry and pharmaceutical chemistry by (Eds), 11th Ed, Lipincott, Raven, Philadelphia, 2004.
• 3. S. N. Pandeya, Textbook of mediacinal chemistry, SG Publ. Varanasi, 2003.

REFERENCES

• 1. D. Abraham (Ed), Burger Medicinal chemistry ad Drug discovery, Vol. 1 & 2. John Wiley & Sons, New York 2003.
• 2. Rama Rao Nadendla, Medicinal Chemistry. R16 B.PHARMACY IV YEAR