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Medicinal Chemistry, 2nd Edition

Book Description

The second edition of Medicinal Chemistry is based on the core module of pharmacy syllabi of various technical universities, and targets undergraduate B.Pharma students across India. The current edition has been designed by authors based on the opinion of the experts to include the latest developments in the field of medicinal chemistry, detailed synthesis mechanism of the drugs and their mode of action inside the body.

Table of Contents

  1. Cover
  2. Title page
  3. Contents
  4. Preface
  5. Chapter 1. Drug Discovery and Development
    1. 1.1 Introduction
    2. 1.2 How are the New Drugs Discovered?
    3. 1.3 Requirements for an Investigational Drug to be Tested in Human Volunteers
    4. 1.4 How are the Investigational Drugs Tested in Humans?
    5. 1.5 How Does Testing Continue after a New Drug is Approved?
    6. 1.6 Procedures Followed in Drug Design
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  6. Chapter 2. Principles of Drug Action
    1. 2.1 Introduction
    2. 2.2 Functional Group Review
    3. 2.3 Stereochemistry
    4. 2.4 Acid-Base Chemistry
    5. 2.5 Biologically Significant Nitrogen-Containing Compounds
    6. 2.6 Physicochemical Properties and Drug Action
    7. 2.7 Bioisosteric Replacement
    8. 2.8 Drug-Receptor Bonding
    9. 2.9 G Protein-Coupled Receptors
    10. Further Readings
    11. Multiple Choice Questions
    12. Questions
    13. Solution to Multiple Choice Questions
  7. Chapter 3. Drug Metabolism and Prodrugs
    1. 3.1 Drug Metabolism
    2. 3.2 Prodrugs
    3. Further Readings
    4. Multiple Choice Questions
    5. Questions
    6. Solution to Multiple Choice Questions
  8. Chapter 4. Computer-aided Drug Design
    1. 4.1 Introduction
    2. 4.2 Cadd Methodology
    3. 4.3 Small Molecule-Based Drug Design
    4. 4.4 Macromolecule-Based Drug Design
    5. 4.5 Substituent Constants Useful for Qsar Analysis
    6. Further Readings
    7. Multiple Choice Questions
    8. Questions
    9. Solution to Multiple Choice Questions
  9. Chapter 5. General Anaesthetics
    1. 5.1 Introduction—Anaesthesia and its Stages
    2. 5.2 Mechanism of Action
    3. 5.3 Classification
    4. 5.4 Inhalation Anaesthetics (Synthesis, Uses, and Dose)
    5. 5.5 Intravenous Anaesthetics (Synthesis, Uses, and Dose)
    6. 5.6 Newer Drugs
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  10. Chapter 6. Local Anaesthetics
    1. 6.1 Introduction
    2. 6.2 Ideal Properties of Local Anaesthetics
    3. 6.3 Mechanism of Action
    4. 6.4 Clinical Uses of Local Anaesthetics
    5. 6.5 Classification of Local Anaesthetics
    6. 6.6 Structures, Synthesis, and Structure-Activity Relationship (Sar) of Benzoic Acid Derivatives
    7. 6.7 Structures, Synthesis, and Sar of P-Aminobenzoic Acid Derivatives
    8. 6.8 Structures, Synthesis, and Sar of Anilides
    9. 6.9 Miscellaneous
    10. 6.10 Newer Drugs
    11. Further Readings
    12. Multiple Choice Questions
    13. Questions
    14. Solution to Multiple Choice Questions
  11. Chapter 7. Sedatives, Hypnotics, and Anxiolytic Agents
    1. 7.1 Introduction
    2. 7.2 Classification of Sedative and Hypnotics
    3. 7.3 Barbiturates
    4. 7.4 Benzodiazepines
    5. 7.5 Benzodiazepine Antagonists
    6. 7.6 Miscellaneous
    7. 7.7 Anxiolytic Agents
    8. 7.8 Newer Drugs
    9. Further Readings
    10. Multiple Choice Questions
    11. Questions
    12. Solution to Multiple Choice Questions
  12. Chapter 8. Anti-Epileptic Drugs
    1. 8.1 Introduction: Epilepsy and Types of Seizures
    2. 8.2 Classification
    3. 8.3 Structural Requirements for Anticonvulsant Agents and Their Structure-Activity Relationship
    4. 8.4 Hydantoins
    5. 8.5 Oxazolidinediones
    6. 8.6 Succinimides
    7. 8.7 Benzodiazepines
    8. 8.8 Gaba Analogues
    9. 8.9 Miscellaneous
    10. 8.10 Newer Anticonvulsants
    11. Further Readings
    12. Multiple Choice Questions
    13. Questions
    14. Solution to Multiple Choice Questions
  13. Chapter 9. Antipsychotic Agents
    1. 9.1 Introduction
    2. 9.2 Typical or Classical Antipsychotic Agents: Synthesis, Mechanism of Action, and Sar
    3. 9.3 Atypical Antipsychotic Agents
    4. 9.4 Newer Drugs
    5. Further Readings
    6. Multiple Choice Questions
    7. Questions
    8. Solution to Multiple Choice Questions
  14. Chapter 10. Antidepressants
    1. 10.1 Introduction
    2. 10.2 Classification
    3. 10.3 Mechanism of Action
    4. 10.4 Side-Effects of Classical Antidepressants
    5. 10.5 Monoamino Oxidase (Mao) Inhibitors
    6. 10.6 Tricyclic Antidepressants
    7. 10.7 Atypical Antidepressants
    8. 10.8 Miscellaneous Drugs
    9. 10.9 Newer Drugs
    10. Further Readings
    11. Multiple Choice Questions
    12. Questions
    13. Solution to Multiple Choice Questions
  15. Chapter 11. Narcotic Analgesics
    1. 11.1 Introduction
    2. 11.2 Mechanism of Action
    3. 11.3 Pharmacophore Requirement
    4. 11.4 Clinical Uses
    5. 11.5 Classification
    6. 11.6 Morphine and its Derivatives
    7. 11.7 Phenyl (Ethyl) Piperidines
    8. 11.8 Diphenyl Heptanones
    9. 11.9 Benzazocin (Benzomorphan) Derivatives
    10. 11.10 Narcotic Antagonists
    11. 11.11 Newer Drugs
    12. Further Readings
    13. Multiple Choice Questions
    14. Questions
    15. Solution to Multiple Choice Questions
  16. Chapter 12. Antipyretics and Non-Steroidal Anti-Inflammatory Drugs
    1. 12.1 Introduction
    2. 12.2 Classification
    3. 12.3 Biosynthesis of Eicosanoids
    4. 12.4 Mechanism of Anti-Inflammatory Action
    5. 12.5 Side-Effects
    6. 12.6 Salicylic Acid Derivatives
    7. 12.7 P-Aminophenol Derivatives
    8. 12.8 Pyrazolidinedione Derivatives
    9. 12.9 Anthranilic Acid Derivatives (Fenamates)
    10. 12.10 Aryl Alkanoic Acid Derivatives
    11. 12.11 Oxicams
    12. 12.12 SAR (Structure Activity Relationship of Oxicams)
    13. 12.13 Miscellaneous Drugs
    14. 12.14 Anti-Gout Drugs
    15. 12.15 Selective Cox-2 Inhibitors
    16. 12.16 Newer Drugs
    17. Further Readings
    18. Multiple Choice Questions
    19. Questions
    20. Solution to Multiple Choice Questions
  17. Chapter 13. Miscellaneous CNS Agents
    1. 13.1 Anti-Parkinsonism Agents
    2. 13.2 Muscle Relaxants
    3. 13.3 Drugs for Alzheimer’s Disease Treatment
    4. 13.4 CNS Stimulants
    5. 13.5 Newer Drugs
    6. Further Readings
    7. Multiple Choice Questions
    8. Questions
    9. Solution to Multiple Choice Questions
  18. Chapter 14. Antihistamines and Anti-Ulcer Agents
    1. 14.1 Introduction
    2. 14.2 H1 Receptor Antagonist
    3. 14.3 H2 Receptor Antagonist
    4. 14.4 Histamine H3 Receptors
    5. 14.5 Histamine H4 Receptors
    6. 14.6 Proton Pump Inhibitors
    7. 14.7 Newer Drugs
    8. Further Readings
    9. Multiple Choice Questions
    10. Questions
    11. Solution to Multiple Choice Questions
  19. Chapter 15. Diuretics
    1. 15.1 Introduction
    2. 15.2 Uses
    3. 15.3 Classification
    4. 15.4 Osmotic Diuretics
    5. 15.5 Carbonic Anhydrase Inhibitors
    6. 15.6 Thiazide Diuretics
    7. 15.7 Potassium-Sparing Diuretics
    8. 15.8 Loop Diuretics
    9. 15.9 Miscellaneous Drugs
    10. 15.10 Newer Drugs
    11. Further Readings
    12. Multiple Choice Questions
    13. Questions
    14. Solution to Multiple Choice Questions
  20. Chapter 16. Antihypertensive Agents
    1. 16.1 Introduction
    2. 16.2 Classification
    3. 16.3 Peripheral Anti-Adrenergic Drugs
    4. 16.4 Centrally Acting Antihypertensive Drugs
    5. 16.5 Direct Vasodilators
    6. 16.6 Ganglionic Blocking Agents
    7. 16.7 β-Adrenergic Blockers
    8. 16.8 Calcium Channel Blockers
    9. 16.9 Angiotensin-Converting Enzyme (Ace) Inhibitors
    10. 16.10 Angiotensin II Antagonists (At2 Antagonists)
    11. 16.11 Miscellaneous Drugs
    12. 16.12 Newer Drugs
    13. Further Readings
    14. Multiple Choice Questions
    15. Questions
    16. Solution to Multiple Choice Questions
  21. Chapter 17. Antiarrhythmic Drugs
    1. 17.1 Introduction
    2. 17.2 Classification
    3. 17.3 Class II Agents
    4. 17.4 Class III Agents
    5. Further Readings
    6. Multiple Choice Questions
    7. Questions
    8. Solution to Multiple Choice Questions
  22. Chapter 18. Antihyperlipidemic Agents
    1. 18.1 Introduction
    2. 18.2 Classification
    3. 18.3 Hmg-Coa Reductase Inhibitors (Statins)
    4. 18.4 Aryloxyisobutyric Acid Derivatives (Fibrates)
    5. 18.5 Miscellaneous Drugs
    6. 18.6 Newer Drugs
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  23. Chapter 19. Antianginal Drugs
    1. 19.1 Introduction
    2. 19.2 Classification
    3. 19.3 Nitrates/Nitrites
    4. 19.4 β-Adrenergic Blockers
    5. 19.5 Calcium Channel Blockers
    6. 19.6 Miscellaneous Drugs
    7. 19.7 Newer Drugs
    8. Further Readings
    9. Multiple Choice Questions
    10. Questions
    11. Solution to Multiple Choice Questions
  24. Chapter 20. Insulin and Oral Hypoglycaemic Agents
    1. 20.1 Introduction
    2. 20.2 Insulin
    3. 20.3 Oral Hypoglycaemic Agents Classification
    4. 20.4 Strategy For Controlling Hyperglycaemia
    5. 20.5 Sulphonyl Ureas
    6. 20.6 Biguanides
    7. 20.7 Substituted Benzoic Acid Derivatives (Meglitinides)
    8. 20.8 Thiazolidinediones
    9. 20.9 Miscellaneous Drugs
    10. 20.10 Newer Drugs
    11. Further Readings
    12. Multiple Choice Questions
    13. Questions
    14. Solution to Multiple Choice Questions
  25. Chapter 21. Oral Anticoagulants
    1. 21.1 Introduction
    2. 21.2 Classification
    3. 21.3 Coumarin Derivatives
    4. 21.4 Indanedione Derivatives
    5. 21.5 Newer Drugs
    6. Further Readings
    7. Multiple Choice Questions
    8. Questions
    9. Solution to Multiple Choice Questions
  26. Chapter 22. Adrenergic Drugs
    1. 22.1 Introduction
    2. 22.2 Sympathomimetic Drugs
    3. 22.3 Sympathetic (Adrenergic) Blocking Agents (Sympatholytics)
    4. 22.4 Newer Drugs
    5. Further Readings
    6. Multiple Choice Questions
    7. Questions
    8. Solution to Multiple Choice Questions
  27. Chapter 23. Cholinergic Drugs
    1. 23.1 Introduction
    2. 23.2 Cholinomimetics
    3. 23.3 Anticholinesterases
    4. 23.4 Cholinergic Blocking Agents (Antimuscarinic Drugs)
    5. 23.5 Newer Drugs
    6. Further Readings
    7. Multiple Choice Questions
    8. Questions
    9. Solution to Multiple Choice Questions
  28. Chapter 24. Sulphonamides, Sulphones, and Dihydrofolate Reductase Inhibitors
    1. 24.1 Sulphonamides
    2. 24.2 Sulphones
    3. 24.3 Dihydrofolate reductase (DHFR) Inhibitors
    4. 24.4 Newer Drug
    5. Further Readings
    6. Multiple Choice Questions
    7. Questions
    8. Solution to Multiple Choice Questions
  29. Chapter 25. Quinolone Antibacterials
    1. 25.1 Introduction
    2. 25.2 Structures of Fluoroquinolones
    3. 25.3 Mechanism of Action
    4. 25.4 Uses
    5. 25.5 Classification
    6. 25.6 SAR of Quinolones
    7. 25.7 Adverse Effects
    8. 25.8 Synthesis of Fluoroquinolones
    9. 25.9 Newer Drugs
    10. Further Readings
    11. Multiple Choice Questions
    12. Questions
    13. Solution to Multiple Choice Questions
  30. Chapter 26. Antibiotics
    1. 26.1 β-Lactam Antibiotics
    2. 26.2 Tetracycline Antibiotics
    3. 26.3 Macrolide Antibiotics
    4. 26.4 Aminoglycoside Antibiotics
    5. 26.5 Miscellaneous Antibiotics
    6. 26.6 Newer Drugs
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  31. Chapter 27. Antitubercular Agents
    1. 27.1 Introduction
    2. 27.2 Mechanisms of Action
    3. Further Readings
    4. Multiple Choice Questions
    5. Questions
    6. Solution to Multiple Choice Questions
  32. Chapter 28. Antifungal Agents
    1. 28.1 Introduction
    2. 28.2 Classification
    3. 28.3 Antifungal Antibiotics
    4. 28.4 Azole Antifungals
    5. 28.5 Pyrimidine Derivatives
    6. 28.6 Miscellaneous Agents
    7. 28.7 Newer Drugs
    8. Further Readings
    9. Multiple Choice Questions
    10. Questions
    11. Solution to Multiple Choice Questions
  33. Chapter 29. Antiviral Agents
    1. 29.1 Anti-HIV Agents
    2. 29.2 Anti-Herpes Simplex Virus (HSV) Agents
    3. 29.3 Miscellaneous Agents
    4. 29.4 Newer Drugs
    5. Further Readings
    6. Multiple Choice Questions
    7. Questions
    8. Solution to Multiple Choice Questions
  34. Chapter 30. Antiprotozoal Agents
    1. 30.1 Introduction
    2. 30.2 Antiamoebic Agents
    3. 30.3 Antimalarial Agents
    4. 30.4 Anthelmintics
    5. 30.5 Miscellaneous Antiprotozoal Drugs
    6. 30.6 Newer Drug
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  35. Chapter 31. Anticancer Agents
    1. 31.1 Introduction
    2. 31.2 Limitations of Therapy
    3. 31.3 Classification
    4. 31.4 Alkylating Agents
    5. 31.5 Antimetabolites
    6. 31.6 Anticancer Antibiotics
    7. 31.7 Miscellaneous Drugs
    8. 31.8 Anticancer Plant Products
    9. 31.9 Hormones and their Antagonists
    10. 31.10 Miscellaneous Drugs
    11. 31.11 Newer Drugs
    12. Further Readings
    13. Multiple Choice Questions
    14. Questions
    15. Solution to Multiple Choice Questions
  36. Chapter 32. Prostaglandins
    1. 32.1 Introduction
    2. 32.2 Functions of Prostaglandins
    3. 32.3 Biosynthesis of Prostaglandins
    4. 32.4 Nomenclature
    5. 32.5 Structures of Therapeutically useful Prostaglandins
    6. 32.6 Sar of Prostaglandins
    7. Further Readings
    8. Multiple Choice Questions
    9. Questions
    10. Solution to Multiple Choice Questions
  37. Chapter 33. Steroids
    1. 33.1 Introduction
    2. 33.2 Biosynthesis of Steroid Hormones
    3. 33.3 Overall Mechanism of Action of Steroid Hormones
    4. 33.4 Oestrogens
    5. 33.5 Progestins
    6. 33.6 Androgens
    7. 33.7 Glucocorticoids
    8. Further Readings
    9. Multiple Choice Questions
    10. Questions
    11. Solution to Multiple Choice Questions
  38. Chapter 34. Miscellaneous Agents
    1. 34.1 Anti-Obesity Drugs
    2. 34.2 Pde-5 Inhibitors for Male Erectile Dysfunction (Ed)
    3. 34.3 Anti-Migraine Drugs
    4. 34.4 Anti-Asthmatics
    5. 34.5 Thyroid and Anti-Thyroid Drugs
    6. 34.6 Anti-Platelet Drugs (Antithrombotics)
    7. 34.7 Immunopharmacological Drugs
    8. 34.8 Anti-Cough and Expectorants
    9. 34.9 Diagnostic Agents
    10. 34.10 Antiseptics and Disinfectants
    11. 34.11 Some Important Antiseptics and Disinfectants
    12. 34.12 Pharmaceutical Aid
    13. 34.13 Vitamins
    14. Further Readings
    15. Multiple Choice Questions
    16. Questions
    17. Solution to Multiple Choice Questions
  39. Chapter 35. Nomenclature of Medicinal Compounds
    1. 35.1 Introduction
    2. 35.2 General Rules
    3. 35.3 Heterocyclic Compounds
    4. 35.4 Examples
    5. Further Readings
    6. Questions
  40. Color Plate Section
  41. Copyright
  42. Back Cover