Textbook of Medicinal Chemistry Vol I book cover

Textbook of Medicinal Chemistry Vol I

Dr Alagarsamy's Textbook of Medicinal Chemistry is a much-awaited masterpiece in its arena. Targeted mainly to B. Pharm. students, this book will also be useful for M. Pharm. as well as M. Sc. organic chemistry and pharmaceutical chemistry students. It aims at eliminating the inadequacies in teaching and learning of medicinal chemistry by providing enormous information on all the topics in medicinal chemistry of synthetic drugs.

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Published: June 2013

Imprint: Elsevier

ISBN: 978-81-312-3258-3

Contents

  • Preface v

    Acknowledgements vii

    Introduction to Medicinal Chemistry

    • Processes of Drug Discovery • Drug Discovery and Design-A

    Historical Outline • Modern Drug Discovery • Screening and

    Designing • Nature as a Source of Drug Compounds

    • Drug Designing

    SECTION I Physicochemical Factors in Relation to Biological Activity of Drugs 9

    Chapter 1 Physicochemical Properties 11

    Chapter 2 Ferguson Principle 13

    Chapter 3 Hydrogen Bonding 15

    Chapter 4 Ionization and pKa Value 19

    Chapter 5 Redox Potential 22

    Chapter 6 Surface Tension 25

    Chapter 7 Complexation 27

    Chapter 8 Steric Features of Drugs 30

    Chapter 9 Bioisosterism 36

    SECTION II Drug Design 41

    Chapter 1 Concepts of Drug Design 43

    • Design of Analogues and Pro-drugs

    • Design of Lead and Lead Discovery • Rational

    Approach to Drug Design

    Chapter 2 Receptors 49

    • Types of Receptors • Theories of Receptors

    • Forces Involved in Drug Receptors Interaction • Factors

    Affecting the Drug-Receptors Interaction

    Chapter 3 Computer-Aided Drug Design 54

    • Bioinformatics Hub

    Chapter 4 Structure-Activity Relationship and

    Quantitative Structure-Activity Relationship 56

    • Historical Development of QSAR

    • Basic Requirements for QSAR Analysis • Model

    Development Procedures

    Chapter 5 Combinatorial Chemistry 66

    • Combinatorial Compound Libraries

    Chapter 6 Pro-Drugs 71

    • Classification of Pro-drugs • Application

    of Pro-drugs

    SECTION III Drugs Acting on Central Nervous System 83

    Chapter 1 Central Nervous System 85

    Chapter 2 Sedatives and Hypnotics 88

    • Molecular Basis of Inhibitory

    Neurotransmitters • Classification • Synthesis and

    Drug Profile • SAR of Barbiturates; SAR of Benzodiazepines

    Chapter 3 General Anaesthetics 130

    • Stages of Anaesthesia • Classification

    • Synthesis and Drug Profile

    Chapter 4 Local Anaesthetics 150

    • Classification • Synthesis and Drug

    Profile • SAR of Benzoic Acid Derivatives • SAR of Anilides

    Chapter 5 Tranquillizers 178

    • General Mode of Action • Classification

    • Synthesis and Drug Profile • SAR of Phenothiazines;

    SAR of Butyrophenones

    Chapter 6 Antidepressants 204

    • Classification • Synthesis and Drug Profile

    • SAR of Dibenzazepines; SAR of Dibenzocylcoheptane

    Derivatives

    Chapter 7 CNS Stimulants 229

    • Classification • Synthesis and Drug Profile

    Chapter 8 Narcotic Analgesics 247

    • Synthesis and Drug Profile

    • SAR of Morphine Derivatives; SAR of Meperidine Analogues;

    SAR of Methadone Derivatives; SAR of Benzomorphan

    Derivatives • Narcotic Antagonists • Classification

    • Synthesis and Drug Profile

    Chapter 9 Anticonvulsants 286

    • Classification • Synthesis and Drug Profile

    • SAR of Hydantoins; SAR of Oxazolidine Diones;

    SAR of Phenacemide Analogues

    Chapter 10 Anti-Prakinsonism Agents 317

    • Classification • Synthesis and Drug Profile

    Chapter 11 Skeletal Muscle Relaxants 329

    • Classification • Synthesis and Drug Profile

    Chapter 12 Alzheimer’s Disease 344

    • Pathogenesis; Treatment

    SECTION IV Drugs Acting on Autonomic Nervous System 349

    Chapter 1 Autonomic Nervous System 351

    Chapter 2 Adrenergic Drugs 356

    • Physiological Basis of Adrenergic Receptors

    Function • General Classification of Adrenergic Agonists

    • Synthesis and Drug Profile • Structural-Activity Relationship

    Chapter 3 Cholinergic Drugs 378

    • Spectrum of Cholinomimetic Drugs

    • Classification • Synthesis and Drug Profile • Structure-

    Activity Relationship

    Chapter 4 Andrenergic Blockers 398

    • Physiological Basis of Adrenergic Receptor

    Antagonists • Classification • Synthesis and Drug Profile

    • Structure-Activity Relationship

    Chapter 5 Anticholinergic Drugs 419

    • Difference Between the Quaternary and

    the Tertiary Antimuscarinics • Classification • Synthesis

    and Drug Profile • SAR of Atropine Analogues; SAR of

    Muscarinic Antagonists

    SECTION V Drugs Acting on Cardiovascular System 445

    Chapter 1 Cardiovascular System 447

    Chapter 2 Antihypertensive Drugs 449

    • Classification • Synthesis and Drug Profile

    Chapter 3 Antiarrhythmic Drugs 476

    • Classification • Synthesis and Drug Profile

    Chapter 4 Antihyperlipidaemic Agents 499

    • Classification • Synthesis and Drug Profile

    Chapter 5 Antianginals 520

    • Principles of Therapy for Angina

    • Classification • Synthesis and Drug Profile • SAR of

    Dihydropyridine Derivatives

    SECTION VI Drugs Acting on Urinary System 547

    Chapter 1 Urinary System 549

    Chapter 2 Diuretics 551

    • Classification • Synthesis and Drug Profile; SAR of Thiazide

    Derivatives; SAR Carbonic Anhydrase Inhibitors; SAR of Loop

    Diuretics

     

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