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
  • 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, 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

  1. 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.
  1. 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.

  1. 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.