BP402T Medicinal Chemistry – I

Unit-I

Introduction to Medicinal Chemistry

• History and development of medicinal chemistry
• Physicochemical properties in relation to biological action
• Ionization, solubility, partition coefficient, hydrogen bonding, protein binding, chelation, bioisosterism, optical and geometrical isomerism
• Drug metabolism: Phase I and Phase II reactions
• Factors affecting drug metabolism including stereochemical aspects

Unit-II

Drugs Acting on Autonomic Nervous System

Adrenergic Neurotransmitters:

• Biosynthesis and catabolism of catecholamines
• Adrenergic receptors (Alpha & Beta) and their distribution
• Sympathomimetic agents: SAR of sympathomimetic agents
• Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine, Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol, Bitolterol, Naphazoline, Oxymetazoline, and Xylometazoline
• Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine
• Mixed mechanism agents: Ephedrine, Metaraminol
  Adrenergic Antagonists:
• Alpha adrenergic blockers: Tolazoline, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide
• Beta adrenergic blockers: SAR of beta blockers, Propranolol, Metipranolol, Atenolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol, Labetalol, Carvedilol

Unit-III

Cholinergic Neurotransmitters

• Biosynthesis and catabolism of acetylcholine
• Cholinergic receptors (Muscarinic & Nicotinic) and their distribution
  Parasympathomimetic Agents:
• SAR of parasympathomimetic agents
• Direct acting agents: Acetylcholine, Carbachol, Bethanechol, Methacholine, Pilocarpine
• Indirect acting (Cholinesterase inhibitors) – Physostigmine, Neostigmine, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathion, Malathion
• Cholinesterase reactivator: Pralidoxime chloride
  Cholinergic Blocking Agents:
• SAR of cholinolytic agents
• Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide
• Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate hydrochloride

Unit-IV

Drugs Acting on Central Nervous System

• General anesthetics
• Inhalation anesthetics: Halothane, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane
• Ultra-short acting barbiturates: Methohexital sodium, Thiamylal sodium, Thiopental sodium
• Dissociative anesthetics: Ketamine hydrochloride
  Narcotic and Non-narcotic Analgesics:
• Morphine and related drugs: SAR of morphine analogues, Morphine sulphate, Codeine, Meperidine hydrochloride, Anileridine hydrochloride, Diphenoxylate hydrochloride, Loperamide hydrochloride, Fentanyl citrate, Methadone hydrochloride, Propoxyphene hydrochloride, Pentazocine, Levorphanol tartrate
• Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartrate, Naloxone hydrochloride
• Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid, Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepirac, Diclofenac, Ketorolac, Ibuprofen, Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone

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, Hammett’s electronic parameter, Taft’s steric parameter, and Hansch analysis
• Pharmacophore modeling and docking techniques
• Combinatorial chemistry: Concept and applications, Solid-phase and solution-phase synthesis.