Additional Information
Book Details
Abstract
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
- Contains clear classification, synthetic schemes, mode of action, metabolism, assay, pharmacological uses with the dose and structure–activity relationship (SAR) of the following classes of drugs:
- Drugs acting on inflammation
- Drugs acting on respiratory system
- Drugs acting on digestive system
- Drugs acting on blood and blood-forming organs
- Drugs acting on endocrine system
- Contains a complete section on chemotherapy and the various classes of chemotherapeutic agents. Also includes recent topics like anti-HIV agents
- Contains brief introduction about the physiological and pathophysiological conditions of diseases and their treatment under each topic
- Provides well-illustrated synthetic schemes and alternative synthetic routes for majority of drugs that help in quick and enhanced understanding of the subject
- Covers the syllabi of majority of Indian universities
Table of Contents
| Section Title | Page | Action | Price |
|---|---|---|---|
| Front Cover\r | Front Cover | ||
| Front Matter\r | i | ||
| Copyright\r | iv | ||
| Preface | v | ||
| Acknowledgements | vii | ||
| Contents | ix | ||
| Section I : Physicochemical Factors In Relation To Biological Activity Of Drugs \r | 9 | ||
| Introduction to Medicinal Chemistry | 1 | ||
| Processes of Drug Discovery | 1 | ||
| Discovery | 1 | ||
| Optimization | 1 | ||
| Development | 2 | ||
| Drug Discovery and Design-A Historical Outline | 2 | ||
| Modern Drug Discovery | 3 | ||
| Targets-New and Established | 3 | ||
| Screening and Designing | 4 | ||
| Nature as a Source of Drug Compounds | 4 | ||
| Plant-Derived Bioactive Materials | 4 | ||
| Microbial Species with Bioactive Metabolites | 5 | ||
| Marine Invertebrates as a Source of Bioactive Compounds | 5 | ||
| Chemical Diversity of Natural Products | 5 | ||
| Methodologies in Natural Product Drug Discovery | 6 | ||
| Identification of Biologically Active Material | 6 | ||
| Structural Elucidation | 6 | ||
| Drug Designing | 6 | ||
| Rational Drug Design | 7 | ||
| Computer-Assisted Drug Design | 7 | ||
| Chapter 1 - Physicochemical Properties | 11 | ||
| Introduction | 11 | ||
| Chapter 2 - Ferguson Principle | 13 | ||
| Introduction | 13 | ||
| Chapter 3 - Hydrogen Bonding | 15 | ||
| Introduction | 15 | ||
| Classification | 15 | ||
| Chapter 4 - Ionization and pKa Value | 19 | ||
| Introduction | 19 | ||
| pKa Value | 19 | ||
| Drug Exerting Action as Undissociated Molecules | 20 | ||
| Drug Exerting Action as Ionized Molecules | 21 | ||
| Chapter 5 - Redox Potential | 22 | ||
| Introduction | 22 | ||
| Chapter 6 - Surface Tension | 25 | ||
| Introduction | 25 | ||
| Classification | 26 | ||
| Applications | 26 | ||
| Chapter 7 - Complexation | 27 | ||
| Introduction | 27 | ||
| Chapter 8 - Steric Features of Drugs | 30 | ||
| Introduction | 30 | ||
| Conformational Isomers | 31 | ||
| Optical Isomers | 32 | ||
| Enantiomers | 32 | ||
| Diastereomers | 33 | ||
| Reasons Behind Varying Activity of Optical Isomers | 34 | ||
| Binding of Enantiomers to Receptors | 35 | ||
| Chapter 9 - Bioisosterism | 36 | ||
| Introduction | 36 | ||
| Classification | 37 | ||
| Section II : Drug Design | 41 | ||
| Chapter 1 - Concepts of Drug Design | 43 | ||
| Introduction | 43 | ||
| Design of Analogues and Prodrugs | 43 | ||
| Design of Lead and Lead Discovery | 44 | ||
| Approaches to Lead Discovery | 44 | ||
| Random Screening | 44 | ||
| Nonrandom Screening | 44 | ||
| Pharmacokinetic Studies | 44 | ||
| Pharmacodynamic Studies | 44 | ||
| Drug Design Through Disjunction | 45 | ||
| Drug Design Through Conjunction | 46 | ||
| Molecular Hybridization in Drug Design | 46 | ||
| Rational Approach to Drug Design | 48 | ||
| Chapter 2 - Receptors | 49 | ||
| Introduction | 49 | ||
| Types of Receptors | 49 | ||
| Theories of Receptors | 50 | ||
| Occupation Theory | 50 | ||
| Rate Theory | 51 | ||
| Induced Fit Theory | 51 | ||
| Macromolecular Perturbation Theory | 51 | ||
| Activation-Aggregation Theory | 52 | ||
| Forces Involved in Drug Receptors Interaction | 52 | ||
| Covalent Bonding | 52 | ||
| Dipole-Dipole and Ion-Dipole Interactions | 52 | ||
| Hydrogen Bonding | 52 | ||
| Electrostatic Bonding | 52 | ||
| Charge Transfer Complex | 53 | ||
| Hydrophobic Forces | 53 | ||
| van der Waal's or London Dispersion Forces | 53 | ||
| Factors Affecting the Drug-Receptor Interaction | 53 | ||
| Chapter 3 - Computer-Aided Drug Design | 54 | ||
| Introduction | 54 | ||
| Bioinformatics Hub | 54 | ||
| Advantages of CADD | 55 | ||
| Chapter 4 - Structure-Activity Relationship and Quantitative Structure-Activity Relationship | 56 | ||
| Introduction | 56 | ||
| Historical Development of QSAR | 57 | ||
| Hansch Analysis | 57 | ||
| Free-Wilson Analysis | 57 | ||
| Mixed Approach | 58 | ||
| Advantages of QSAR | 58 | ||
| Disadvantages of QSAR | 58 | ||
| Basic Requirements for QSAR Analysis | 58 | ||
| Steps Involved in QSAR Studies | 59 | ||
| Statistical Methods Used in QSAR Analysis | 59 | ||
| Regression Methods | 59 | ||
| Partial Least Square (PLS) | 59 | ||
| Genetic Function Approximation (GFA) | 60 | ||
| Genetic Partial Least Squares (G/PLSs) | 60 | ||
| Principal Component Analysis (PCA) | 60 | ||
| Statistical Measures Commonly Used in Regression Analysis | 60 | ||
| Model Development Procedures | 61 | ||
| Classical or 2D QSAR Analysis | 61 | ||
| 3D-QSAR Analysis | 62 | ||
| Comparative Molecular Field Analysis (CoMFA) | 62 | ||
| Comparative Molecular Similarity Indices Analysis (CoMSIA) | 64 | ||
| Chapter 5 - Combinatorial Chemistry | 66 | ||
| Introduction | 66 | ||
| Principles of Combinatorial Chemistry | 66 | ||
| Combinatorial Compound Libraries | 67 | ||
| Combinatorial Synthesis on Solid Phase | 67 | ||
| Advantages and Disadvantages of Solid Support Reagents | 68 | ||
| Resins for SPS | 68 | ||
| Chapter 6 - Pro-Drugs | 71 | ||
| Introduction | 71 | ||
| Ideal Properties | 71 | ||
| Classification of Pro-Drug | 71 | ||
| Applications of Pro-Drug | 75 | ||
| Improvement of Taste | 76 | ||
| Improvement of Odour | 76 | ||
| Enhancement of Bio-Availability (Lipophilicity) | 76 | ||
| Improvement of Stability and Solubility | 77 | ||
| Decreased Toxicity and Adverse Reactions | 77 | ||
| Site-Specific Drug Delivery | 78 | ||
| Increased duration of action | 78 | ||
| Bio-Precursor Prodrug | 78 | ||
| Section III : Drugs Acting Oncentral Nervoussystem\r | 83 | ||
| Chapter 1 - Central Nervous System | 85 | ||
| Introduction | 85 | ||
| Amino Acids | 85 | ||
| Adrenergic Pathway in CNS | 86 | ||
| Functional Aspects of Dopamine | 86 | ||
| Functional Aspects of 5-HT | 86 | ||
| Cholinergic Transmission in CNS | 86 | ||
| Other Neurotransmitters and Functions in CNS | 86 | ||
| Chapter 2 - Sedatives and Hypnotics | 88 | ||
| Introduction | 88 | ||
| Treatment of Anxiety States | 89 | ||
| Treatment of Sleep Problems | 89 | ||
| Other Therapeutic Uses | 89 | ||
| Molecular Basis of Inhibitory Neurotransmitters | 89 | ||
| Classification | 89 | ||
| Synthesis and Drug Profile | 96 | ||
| SAR of Barbiturates | 106 | ||
| SAR of Benzodiazepines | 116 | ||
| Chapter 3 - General Anaesthetics | 130 | ||
| Introduction | 130 | ||
| Types of General Anaesthetics | 130 | ||
| Stages of Anaesthesia | 131 | ||
| Classification | 131 | ||
| Synthesis and Drug Profile | 134 | ||
| Chapter 4 - Local Anaesthetics | 150 | ||
| Introduction | 150 | ||
| Classification | 151 | ||
| Synthesis and Drug Profile | 154 | ||
| Sar of Benzoic Acid Derivatives | 164 | ||
| SAR of Anilides | 170 | ||
| Chapter 5 - Tranquillizers\r | 178 | ||
| Introduction | 179 | ||
| General Mode of Action | 179 | ||
| Classification | 179 | ||
| -->Synthesis and drug profile | 183 | ||
| SAR of Phenothiazines | 188 | ||
| SAR of Butyrophenones | 194 | ||
| Chapter 6 - Antidepressants\r | 204 | ||
| Introduction | 205 | ||
| Uses | 205 | ||
| Classification | 206 | ||
| Synthesis and drug profile | 209 | ||
| SAR of Dibenzazepines | 216 | ||
| -->SAR of Dibenzo Cycloheptane Derivatives | 219 | ||
| Chapter 7 - CNS Stimulants\r | 229 | ||
| Introduction | 229 | ||
| Classification | 229 | ||
| Synthesis and Drug Profile | 233 | ||
| Xanthine Derivatives | 239 | ||
| Chapter 8 - Narcotic Analgesics | 247 | ||
| Introduction | 247 | ||
| Opioid Analgesics | 247 | ||
| General Mode of Action | 248 | ||
| Therapeutic Uses | 249 | ||
| Classification | 249 | ||
| Synthesis and Drug Profile | 254 | ||
| SAR of morphine | 259 | ||
| SAR of Meperidine Analogues | 269 | ||
| SAR of Diphenyl Heptanone (Methadone Series) | 273 | ||
| SAR of Benzomorphan Derivatives (Benzazocines) | 276 | ||
| Narcotic Antagonists | 278 | ||
| Classification | 278 | ||
| Chapter 9 - Anticonvulsants | 286 | ||
| Introduction | 286 | ||
| Classification | 287 | ||
| Pharmalocogical Classification | 291 | ||
| Synthesis and Drug Profile | 291 | ||
| SAR of Barbiturates | 293 | ||
| SAR of Hydantoins | 295 | ||
| SAR of Oxazolidinediones | 298 | ||
| SAR of Succinimides | 301 | ||
| SAR of Phenacemide | 302 | ||
| SAR of Sodium Valproate | 309 | ||
| Chapter 10 - Antiparkinsonism Agents | 317 | ||
| Introduction | 317 | ||
| Classification | 319 | ||
| Synthesis and Drug Profile | 322 | ||
| Chapter 11 - Skeletal Muscle Relaxants | 329 | ||
| Introduction | 329 | ||
| Classification | 331 | ||
| Synthesis and Drug Profile | 333 | ||
| Chapter 12 - Alzheimers Disease | 344 | ||
| Introduction | 344 | ||
| Pathogenesis | 344 | ||
| Treatment | 345 | ||
| Acetylcholinesterase Inhibitors | 345 | ||
| NMDA Antagonists | 345 | ||
| Tacrine | 345 | ||
| Section IV : Drugs Acting Onautonomic Nervoussystem \r | 349 | ||
| Chapter 1 - Autonomic Nervous System | 351 | ||
| Introduction | 351 | ||
| Sympathetic System | 351 | ||
| Neurotransmission | 351 | ||
| Regulation of Catecholamines | 352 | ||
| Adrenergic Receptors | 352 | ||
| Chapter 2 - Adrenergic Drugs | 356 | ||
| Introduction | 356 | ||
| Physiological Basis of Adrenergic Receptor Function | 356 | ||
| Mechanism of Action of Sympathomimetics | 357 | ||
| Chapter 3 - Cholinergic Drugs | 378 | ||
| Introduction | 378 | ||
| Spectrum of Cholinomimetic Drugs | 378 | ||
| Direct-acting Cholinoceptor Stimulants | 378 | ||
| Mechanism of Action of Directly Acting Cholinergic Drugs | 378 | ||
| Indirect Acting Cholinomimetic Drugs | 379 | ||
| Mechanism of Action of Indirectly Acting Cholinergic Drugs (Anticholinesterase Agents) | 379 | ||
| Classification | 380 | ||
| Synthesis and Drug Profile | 383 | ||
| Structure Activity Relationship | 396 | ||
| Chapter 4 - Adrenergic Blockers | 398 | ||
| Introduction | 398 | ||
| Physiological Basis of Adrenergic Receptor Antagonists | 398 | ||
| Mechanism of Action of -Adrenergic Blockers | 399 | ||
| Mechanism of Action of -Adrenergic Receptor Blockers | 399 | ||
| Classification | 399 | ||
| Synthesis and Drug Profile | 403 | ||
| Structure-Activity Relationship | 418 | ||
| Chapter 5 - Anticholinergic Drugs | 419 | ||
| Introduction | 419 | ||
| Difference Between the Quaternary and the Tertiary Antimuscarinics | 420 | ||
| Quaternary Amines | 420 | ||
| Tertiary Amines | 420 | ||
| Therapeutic Uses | 420 | ||
| Classification | 421 | ||
| Synthesis and Drug Profile | 425 | ||
| SAR Solanaceous Alkaloids (Atropine Analogues) | 428 | ||
| SAR of Muscarinic Antagonists | 440 | ||
| Section V : Drugs Acting Oncardiovascularsystem \r | 445 | ||
| Chapter 1 - Cardiovascular System | 447 | ||
| Introduction | 447 | ||
| Aetiology of Hypertension | 447 | ||
| Normal Regulation of Blood Pressure | 448 | ||
| Chapter 2 - Antihypertensive Drugs | 449 | ||
| Introduction | 449 | ||
| Hypertension | 449 | ||
| Primary Hypertension | 449 | ||
| Secondary Hypertension | 449 | ||
| Classification | 450 | ||
| Synthesis and Drug Profile | 463 | ||
| Chapter 3 - Antiarrhythmic Drugs | 476 | ||
| Introduction | 476 | ||
| Classification | 477 | ||
| Synthesis and Drug Profile | 481 | ||
| Chapter 4 - Antihyperlipidaemic Agents | 499 | ||
| Introduction | 499 | ||
| Classification | 500 | ||
| Synthesis and Drug Profile | 505 | ||
| Chapter 5 - Antianginals | 520 | ||
| Introduction | 520 | ||
| Principles of Therapy for Angina | 520 | ||
| Classification | 521 | ||
| Synthesis and Drug Profile | 526 | ||
| Sar of Dihydropyridines | 537 | ||
| Second-Generation Alkyl Amine Type Calcium Channel Blockers | 540 | ||
| Section VI : Drugs Acting Onurinary System\r | 547 | ||
| Chapter 1 - Urinary System | 549 | ||
| Introduction | 549 | ||
| Functions of Renal System | 549 | ||
| Principle of Glomerular Filtration | 550 | ||
| Principle of Tubular Reabsorption and Secretion | 550 | ||
| Chapter 2 - Diuretics | 551 | ||
| Introduction | 551 | ||
| Classification | 552 | ||
| Synthesis and Drug Profile | 558 | ||
| SAR of Thiazide Diruretics | 567 | ||
| SAR of CAse Inhibitiors | 571 | ||
| SAR of Loop Diuretics | 583 | ||
| Properties | 585 | ||
| Index | 591 | ||
| A | 591 | ||
| B | 592 | ||
| C | 593 | ||
| D | 594 | ||
| E | 595 | ||
| F | 595 | ||
| G | 596 | ||
| H | 596 | ||
| I | 597 | ||
| K | 597 | ||
| L | 597 | ||
| M | 598 | ||
| N | 599 | ||
| O | 600 | ||
| P | 600 | ||
| Q | 601 | ||
| R | 601 | ||
| S | 602 | ||
| T | 603 | ||
| U | 603 | ||
| V | 604 | ||
| W | 604 | ||
| X | 604 | ||
| Z | 604 |