MEDICINAL CHEMISTRY – I BP402T - PUBLIC HEALTH PHARMACY

MEDICINAL CHEMISTRY – I BP402T

Study of the development of the following classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted (*).

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
Drug metabolism principles- Phase I and Phase II.
Factors affecting drug metabolism including stereo chemical aspects.

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*, Metipranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol, Carvedilol.

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, 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, Clidinium bromide, Dicyclomine hydrochloride*, Glycopyrrolate, Methantheline bromide, Propantheline bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride, Procyclidine hydrochloride*, Tridihexethyl chloride, Isopropamide iodide, Ethopropazine hydrochloride.

Drugs acting on Central Nervous System
A. 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: Glutethimide.
Alcohol & their carbamate derivatives: Meprobamate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.
B. Antipsychotics
Phenothiazines: SAR of Phenothiazines- Promazine hydrochloride, Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine hydrochloride, Prochlorperazine maleate, Trifluoperazine hydrochloride.
Ring Analogues of Phenothiazines: Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine.
Fluoro buterophenones: Haloperidol, Droperidol, Risperidone.
Beta amino ketones: Molindone hydrochloride.
Benzamides: Sulpiride.
C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action.
Barbiturates: Phenobarbitone, Metharbital.
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.

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, 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.