Medicinal Chemistry 1
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 stereo chemical aspects.
Unit: 2 (Part-1)
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: 2 (Part-2)
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: 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, Parathione, 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
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.
2. 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.
- 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 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.
