UNIT 1:
Introduction to Medicinal Chemistry
History and development of medicinal chemistry
Hydrogen bonding, Protein binding,
Optical and Geometrical isomerism.
Optical and Geometrical isomerism.
Drug metabolism principles- Phase I
Drug metabolism principles- Phase II
Factors affecting drug metabolism including stereo chemical aspects. UNIT- II 1
UNIT 2:
Adrenergic Neurotransmitters: Biosynthesis and catabolism of catecholamine.
UNIT 3:
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,
UNIT 4:
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 5:
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.
