Medicinal Chemistry - I
Unit I: Introduction to Medicinal Chemistry (10 hours)
- 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 principles: Phase I and Phase II
- Factors affecting drug metabolism including stereo chemical aspects
Unit II: Drugs acting on Autonomic Nervous System (10 hours)
- 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 (10 hours)
- 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 (08 hours)
- Sedatives and Hypnotics: Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam*, Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem
- Barbiturates: SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital
- Miscellaneous: Amides & imides: Glutethmide. Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol. Aldehyde & their derivatives: Triclofos sodium, Paraldehyde
- 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.
- 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 (07 hours)
- 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, 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.