B.Pharmacy 4th Semester Medicinal Chemistry-I Notes

Medicinal Chemistry–I notes for B.Pharmacy 4th semester cover principles of drug design, structure–activity relationships, physicochemical properties, synthesis, mechanisms of action, and therapeutic applications of drugs. These notes help students understand how chemical structure influences biological activity, metabolism, and safety, forming a strong foundation for advanced medicinal chemistry and pharmaceutical studies.

Bachelor of Pharmacy
Semester		4th Semester		Subject		Medicinal Chemistry – I
Syllabus
Unit 1st	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.
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Unit 2nd	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, and propylhexedrine. Agents with mixed mechanisms: 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.
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Unit 3rd	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, and 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 Glycopyrrolate, bromide, Dicyclomine Methantheline bromide, hydrochloride, Propantheline bromide, Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride, Procyclidine hydrochloride, Tridihexethyl chloride, Isopropamide iodide, Ethopropazine hydrochloride.
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Unit 4th	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 Miscelleneous: Amides & imides: Glutethmide. Alcohol & their carbamate derivatives: Meprobomate, 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 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
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Unit 5th	Drugs acting on Central Nervous System General anesthetics: Inhalation anaesthetics: 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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Medicinal Chemistry–I focuses on the chemical basis of drug action and the relationship between chemical structure and biological activity. It covers drug design principles, physicochemical properties, and structure–activity relationships (SAR). The subject includes detailed study of important drug classes, their synthesis, mechanisms of action, metabolism, and therapeutic uses, helping students understand how chemical modifications influence pharmacological activity and safety.

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