4th Semester Medicinal Chemistry Notes

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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 II

• Factors affecting drug metabolism including stereochemical 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

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, Parathion, 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

• 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

Miscellaneous:

• Amides & imides: Glutethmide.
• Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
• Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.

Antipsychotics

• Phenothiazines: 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.

. 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 barbiturates: 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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