Medicinal Chemistry 1
Handwritten Notes
Syllabus:
Unit 1
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 IIFactors affecting drug metabolism including stereo chemical aspects.
Unit 2
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 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
Synthetic cholinergic blocking agents: 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 4
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 5
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.
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