Medicinal Chemistry 1 Notes pdf
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Introduction to Medicinal Chemistry
History and development of medicinal chemistryPhysicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein
binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
Medicinal chemistry 1 (UNIT-2)
Drugs acting on Autonomic Nervous System
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.
Alpha adrenergic blockers: Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide.
Beta adrenergic blockers: SAR of beta blockers, Propranolol*,
Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol,
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.
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
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
Phensuximide, Methsuximide, Ethosuximide* Urea and monoacylureas: Phenacemide, Carbamazepine*
Benzodiazepines: Clonazepam Miscellaneous: Primidone, Valproic acid , Gabapentin, Felbamate
Other Subjects Notes Given below :
Drugs acting on Central Nervous System General anesthetics:
Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane. Ultra short acting barbitutrates: Methohexital sodium*, Thiamylalsodium, 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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