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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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