Medicinal Chemistry – I Free Notes Download – B. Pharm

Unit I

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

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Drug metabolism

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

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Unit II

Drugs acting on Autonomic Nervous System Adrenergic Neurotransmitters

Biosynthesis and catabolism of catecholamine.
Adrenergic receptors (Alpha & Beta) and their distribution

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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

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Adrenergic Antagonists

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Alpha adrenergic blockers

Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide

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Beta adrenergic blockers

SAR of beta blockers, Propranolol*, Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol, Carvedilol

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Unit III

Cholinergic neurotransmitters

Biosynthesis and catabolism of acetylcholine.
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution
.

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Parasympathomimetic agents

SAR of Parasympathomimetic agents
Direct acting agents

Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine

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Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible)

Physostigmine, Neostigmine*, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion

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Cholinesterase reactivator

Pralidoxime chloride

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Cholinergic Blocking agents

SAR of cholinolytic agents

Solanaceous alkaloids and analogues

Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide

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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

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Unit IV

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

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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

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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

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Unit V

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

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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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