JAWAHARLAL NEHRU TECHNOLOGICAL UNIVERSITY HYDERABAD

Course Objectives

The basic consideration of drug activity, drug metabolism and medicinal

substances belonging to different categories are discussed in an elaborative manner. The synthesis and mechanism of action of the medicinal compounds are explained in an organized way which helps the students to understand the medicinal uses of the compounds.

Course Outcome

The students gain good knowledge about the usage of medicinal substances, the

synthesis and drug-drug interactions, so that they can get involved with confidence in the patient counseling.

UNIT - I

• a. Basic considerations of Drug activity: Physico chemical properties of drug molecules in relation to biological activity – Solubility, lipophilicity, partition-coefficient, Ionization, hydrogen bonding, Chelation, redox potential and surface activity. Bioisosterism and steric features of drugs, drug distribution and protein binding: Introduction to Pro and soft drug approaches.
• b. Drug metabolism and inactivation: Introduction, Phase-I and Phase-II reactions.

Note

Introduction, definition, nomenclature, chemical classification, structure, synthesis,

general mechanism, and mode of action, SAR including physicochemical and stereo chemical aspects, metabolism and therapeutic uses of the drugs from each category shall be studied for the following units. An outline of synthetic procedure of only the drugs mentioned in each category.

UNIT - II

Drugs acting on CNS: A brief study of the chemistry of neurotransmitters.

• a. Hypnotics and Anxiolytics: Phenobarbital, diazepam, alprazolam, glutethimide Anti-psychotics: Chlorpromazine, haloperidol, clozapine, oxypentine. Anti-epileptics: Phenytoin, valproic acid, carbamazepine, ethosuximide. Anti-depressants: Imipramine, fluoxetine, doxepine
• b. Local anesthetic and General anesthetic agents: benzocaine, procaine, dibucaine and lidocaine, halothane and thiopental sodium.

UNIT - III

• a. Adrenergic agents and adrenergic blockers.Isoproterenol, atenolol, henoxybenzamine, amphetamine, ephedrine, salbutamol,
• b. Cholinergic agents and acetyl cholinesterase inhibitors Cholinergics: Carbachol, bethanichol Anticholinesterase: Neostigmine, pyridostigmine Neuromuscular blockers: succinyl choline.
• c. Anti-cholinergics: atropine, ipratropium bromide, dicyclomine, bipyridine, propantheline

UNIT - IV

• a. Prostaglandins. Introduction, nomenclature, functions,bio synthesis of prostaglandin E1, Structures of clinically useful prostaglandins.
• b. Analgesics and NSAIDS (Non-steroidal anti-inflamatory agents):
• i. Introduction and types of pain and inflammation ii Classification and systematic development of analgesics of morphine, mild analgesics and strong analgesics: Meperidine and Methadone
• iii. NSAIDS – Aspirin, paracetamol, oxyphenbutazone, ibuprofen, indomethacin, diclofenac and meloxicam
• iv. A brief account on Cox-2 inhibitors and nimsulide.

UNIT - V

General account of cardiovascular diseases

• a. Antihypertensives: methyldopa, amlodipine, enalapril, losartan.
• b. Anti-arrhythmics: procainamide
• c. Diuretics: acetazolamide, hydrochlorthiazide, furosemide
• d. Anticoagulants, Anti-anginals and Coronary vasodilators: Isosorbide dinitrate, verapamil, diltiazem

TEXT BOOKS:

• 1. William O. Foye, Textbook of Medicinal Chemistry, Lea Febiger, Philadelphia.
• 2. JH Block & JM Beale (Eds), Wilson & Giswold’s Text book of organic Medicinal Chemistry and th pharmaceutical chemistry, 11 Ed, Lipcott, Raven, Philadelphia, 2004.
• 3. Medicinal Chemistry by Korol Kavas.

REFERENCES

• 1. D. Abraham (Ed), Burger Medicinal chemistry ad Drug discovery, Vol. 1 & John Wiley & Sons, th New York 2003, 6 Ed.
• 2. Daniel lednicer, Strategies for Organic Drug Synthesis and Design, John Wiley, N. Y. 1998.