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A Textbook of Medicinal Chemistry – I


  • ISBN: 9789395596091
  • Published : November 2022
  • Book Language : English
  • Edition : First
  • Format : Paperback
  • Pages : 267
  • Category:
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A Textbook of Medicinal Chemistry – I

This book is the best book of Medicinal Chemistry-I for S.Y.B.Pharmacy, Sem.IV as per Pharmacy Council of India, New Delhi which deals classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs.
This Medicinal Chemistry-I content five units, Ist unit content Introduction to Medicinal Chemistry, History and development of medicinal chemistry, physicochemical properties in relation to biological action and Drug metabolism.Unit IInd content Drugs acting on Autonomic Nervous System- Adrenergic Neurotransmitters and Adrenergic Antagonists. Unit-IIIrd consist of Cholinergic neurotransmitters-Parasympathomimetic agents and Cholinergic Blocking agents. Unit IVth content Drugs acting on Central Nervous System- A. Sedatives and Hypnotics, B. Antipsychotics C. Anticonvulsants Unit-Vth Drugs acting on Central Nervous System-General Anesthetics, Narcotic and non-narcotic analgesics.

1. Introduction to Medicinal Chemistry 
A. History and development of medicinal chemistry
B. Physicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
C. Drug metabolism – Drug metabolism principles-Phase I and Phase II. Factors affecting drug metabolism including stereo chemical aspects.

2. Drugs Acting on Autonomic Nervous System 
A. Adrenergic Neurotransmitters :
• Biosynthesis and catabolism of catecholamine.
• Adrenergic receptors (Alpha & Beta) and their distribution.
B. 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.

3. Cholinergic Neurotransmitters 
A. Cholinergic Neurotransmitters :
• Biosynthesis and catabolism of acetylcholine.
• Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
B. 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.

4. 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.

5. Drugs Acting on Central Nervous System
A. General Anesthetics :
• Inhalation Anesthetics : Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane.
• Ultra short acting barbitutrates : Methohexital sodium*, Thiamylal sodium, Thiopental sodium.
• Dissociative anesthetics : Ketamine hydrochloride.*


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