1. Introduction to Medicinal Chemistry
1. Introduction to Medicinal Chemistry.
2. History and development of medicinal chemistry.
3. Physicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
4. Drug metabolism :
i) Drug metabolism principles - Phase I and Phase II.
ii) Factors affecting drug metabolism including stereo chemical aspects.
2. Drugs Acting on Autonomic Nervous System
1. Adrenergic Neurotransmitters :
i) Biosynthesis and catabolism of catecholamine.
ii) Adrenergic receptors (Alpha & Beta) and their distribution.
2. Sympathomimetic agents : SAR of Sympathomimetic agents
i) Direct acting : Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.
ii) Indirect acting agents : Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.
iii) Agents with mixed mechanism : Ephedrine, Metaraminol.
3. Adrenergic Antagonists :
i) Alpha adrenergic blockers : Tolazoline*, Phentolamine, Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide.
ii) Beta adrenergic blockers : SAR of beta blockers, Propranolol*, Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol, Carvedilol.
3. Cholinergic and Anticholinergic Drugs
1. Cholinergic neurotransmitters :
Biosynthesis and catabolism of acetylcholine.
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
2. Parasympathomimetic agents :
SAR of Parasympathomimetic agents,
i) Direct acting agents : Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine.
ii) Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible) :
Physostigmine, Neostigmine*, Pyridostigmine, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion.
iii) Cholinesterase reactivator : Pralidoxime chloride.
3. Cholinergic Blocking agents : SAR of cholinolytic agents
i) Solanaceous alkaloids and analogues :
Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine hydrobromide, Ipratropium bromide*.
ii) 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.
4. Drugs Acting on Central Nervous System
1. Sedatives and Hypnotics :
i) Benzodiazepines : SAR of Benzodiazepines, Chlordiazepoxide, Diazepam*, Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem
ii) Barbiturtes : SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital.
iii) Miscelleneous :
Amides & imides : Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives : Triclofos sodium, Paraldehyde.
2. Antipsychotics :
i) Phenothiazeines : SAR of Phenothiazeines - Promazine hydrochloride, Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine hydrochloride, Prochlorperazine maleate, Trifluoperazine hydrochloride.
ii) Ring Analogues of Phenothiazeines : Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine.
iii) Fluro buterophenones : Haloperidol, Droperidol, Risperidone.
iv) Beta amino ketones : Molindone hydrochloride.
v) Benzamides : Sulpieride.
3. Anticonvulsants : SAR of Anticonvulsants, mechanism of anticonvulsant action
i) Barbiturates : Phenobarbitone, Methabarbital.
ii) Hydantoins : Phenytoin*, Mephenytoin, Ethotoin
iii) Oxazolidine diones : Trimethadione, Paramethadione
iv) Succinimides : Phensuximide, Methsuximide, Ethosuximide*
v) Urea and monoacylureas : Phenacemide, Carbamazepine*
vi) Benzodiazepines : Clonazepam
vii) Miscellaneous : Primidone, Valproic acid , Gabapentin, Felbamate.
5. Drugs Acting on Central Nervous System
1. General Anesthetics :
i) Inhalation anesthetics : Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane.
ii) Ultra short acting barbitutrates : Methohexital sodium*, Thiamylal sodium, Thiopental sodium.
iii) Dissociative anesthetics : Ketamine hydrochloride.*
2. Narcotic and Non-narcotic Analgesics :
i) 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.
ii) Narcotic antagonists : Nalorphine hydrochloride, Levallorphan tartarate, Naloxone hydrochloride.
iii) Anti-inflammatory agents : Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac, Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone.
