SYLLABUS OF MEDICINAL CHEMISTRY 1st (4th sem Bpharm)

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                                             SUBJECT

                         MEDICINAL CHEMISTRY-1st

                               (SUB CODE-BP402T,4th Sem Bpharm,PCI)


UNIT- I 

  • 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- II   

  • 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.
  • 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-III 

  • 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
  • Solanaceous alkaloids and analogues: 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- IV 

  • Drugs acting on Central Nervous System

  • A. 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.
  • B. 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.
  • 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

UNIT – V 

  • 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.

                     

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