“Medicinal Chemistry–I” is a comprehensive and student-friendly book that provides a clear understanding of the fundamental concepts of medicinal chemistry in a simple and systematic manner. The book is designed to help readers grasp the essential principles of drug design, classification, mechanism of action, and therapeutic applications with clarity and ease.
The text begins with an introduction to medicinal chemistry, covering its history, development, and the significance of physicochemical properties such as solubility, ionization, and protein binding in relation to biological activity. It also explains the principles of drug metabolism, including Phase I and Phase II reactions and factors influencing metabolic processes.
The book further explores drugs acting on the autonomic nervous system, detailing adrenergic and cholinergic neurotransmitters, their receptors, and structure–activity relationships of important drug classes. It provides a systematic study of sympathomimetic and parasympathomimetic agents, along with cholinergic blocking agents and their pharmacological significance.
In addition, the content covers drugs acting on the central nervous system, including sedatives, hypnotics, antipsychotics, anticonvulsants, and anesthetics. Key drug categories are discussed with emphasis on their chemical structures, mechanisms, and therapeutic uses, enabling a strong conceptual understanding.
With its structured presentation and focus on both theoretical and practical aspects, this book serves as a valuable resource for building a solid foundation in medicinal chemistry and supports learners in understanding the relationship between chemical structure and biological activity.
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.*
A book as per the latest syllabus given by Pharmacy Council of India (PCI) New Delhi
for B.Pharm students of all Indian Universities