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.
Salient Features
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