SYLLABUS
Unit-I
Introduction to Medicinal Chemistry
History and development of medicinal chemistry
Physico-chemical properties in relation to biological action
Ionization, solubility, partition coefficient, hydrogen bonding, protein binding, chelation, bioisosterism,
optical and geometrical isomerism.
Drug metabolism
Drug metabolism principles- Phase-I and Phase-II. Factors affecting drug metabolism including stereochemical aspects.
Unit-II
Drugs acting on Autonomic Nervous System
Adrenergic Neurotransmitters
Biosynthesis and catabolism of catecholamine.
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.
• Agents with mixed mechanism: Ephedrine, metaraminol.
Adrenergic Antagonists:
Alpha adrenergic blockers: Tolazoline*, phentolamine, phenoxybenzamine, prazosin, dihydroergotamine,
methysergide.
Beta adrenergic blockers: SAR of beta blockers, propranolol*, metibranolol, atenolol, betazolol,
bisoprolol, esmolol, metoprolol, labetolol, 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 (reversible & irreversible): Physostigmine, neostigmine*,
pyridostigmine, edrophonium chloride, tacrine hydrochloride, ambenonium chloride, isofluorphate,
echothiophate iodide, parathione, 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, clidinium
bromide, dicyclomine hydrochloride*, glycopyrrolate, methantheline bromide, propantheline bromide,
benztropine mesylate, orphenadrine citrate, biperidine hydrochloride, procyclidine hydrochloride*,
tridihexethyl chloride, isopropamide iodide, ethopropazine hydrochloride.
Unit-IV
Drugs acting on Central Nervous System
A. Sedatives and Hypnotics:
Benzodiazepines: SAR of benzodiazepines, chlordiazepoxide, diazepam*, oxazepam, chlorazepate,
lorazepam, alprazolam, zolpidem.
Barbiturtes: SAR of barbiturates, barbital*, phenobarbital, mephobarbital, amobarbital, butabarbital,
pentobarbital, secobarbital.
Miscelleneous:
Amides & imides: Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, paraldehyde.
B. Antipsychotics
Phenothiazeines: SAR of Phenothiazeines - Promazine hydrochloride, chlorpromazine hydrochloride*,
triflupromazine, thioridazine hydrochloride, piperacetazine hydrochloride, prochlorperazine maleate,
Trifluoperazine hydrochloride.
Ring Analogues of Phenothiazeines: Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine.
Fluro buterophenones: Haloperidol, Droperidol, Risperidone.
Beta amino ketones: Molindone hydrochloride.
Benzamides: Sulpieride.
C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action
Barbiturates: Phenobarbitone, Methabarbital.
Hydantoins: Phenytoin*, Mephenytoin, Ethotoin
Oxazolidine diones: Trimethadione, Paramethadione
Succinimides: Phensuximide, methsuximide, ethosuximide* urea and
monoacylureas: Phenacemide, carbamazepine*
Benzodiazepines: Clonazepam
Miscellaneous: Primidone, valproic acid , Gabapentin, Felbamate.
Unit-V
Drugs acting on Central Nervous System
General anesthetics:
Inhalation anesthetics: Halothane*, methoxyflurane, enflurane, sevoflurane, isoflurane, desflurane.
Ultra short acting barbitutrates: 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, Anilerdine hydrochloride, diphenoxylate hydrochloride, loperamide hydrochloride,
fentanyl citrate*, methadone hydrochloride*, propoxyphene hydrochloride, pentazocine, levorphanol
tartarate.
Narcotic antagonists: Nalorphine hydrochloride, levallorphan tartarate, naloxone hydrochloride.
Anti-inflammatory agents: Sodium salicylate, aspirin, mefenamic acid*, meclofenamate, indomethacin,
sulindac, tolmetin, zomepriac, diclofenac, ketorolac, ibuprofen*, naproxen, piroxicam, phenacetin,
acetaminophen, antipyrine, phenylbutazone.