Medicinal Chemistry I Syllabus PDF | B.Pharm 4th Semester | Old Syllabus

Medicinal Chemistry I syllabus for 4th Semester. This page presents the detailed syllabus content from the original Old Syllabus PDF.

About This Syllabus

Physicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein
binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.

Course Syllabus

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

Unit- Ii 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-Iii 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 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

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 – 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.* 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. BP406P. MEDICINAL CHEMISTRY – I (Practical) I Preparation of drugs/ intermediates 1 1,3-pyrazole 2 1,3-oxazole 3 Benzimidazole 4 Benztriazole 5 2,3- diphenyl quinoxaline 6 Benzocaine 7 Phenytoin 8 Phenothiazine 9 Barbiturate II Assay of drugs 1 Chlorpromazine 2 Phenobarbitone 3 Atropine 4 Ibuprofen 5 Aspirin 6 Furosemide III Determination of Partition coefficient for any two drugs

Practical Syllabus

BP406P. MEDICINAL CHEMISTRY – I (Practical)

I Preparation of drugs/ intermediates 1 1,3-pyrazole 2 1,3-oxazole 3 Benzimidazole 4 Benztriazole 5 2,3- diphenyl quinoxaline 6 Benzocaine 7 Phenytoin 8 Phenothiazine 9 Barbiturate

II Assay of drugs 1 Chlorpromazine 2 Phenobarbitone 3 Atropine 4 Ibuprofen 5 Aspirin 6 Furosemide

III Determination of Partition coefficient for any two drugs

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