Medicinal Chemistry

Description

Cover Medicinal Chemistry Copyright Contents Preface Drug Discovery and Development Introduction How are the New Drugs Discovered? Requirements for an Investigational Drug to be Tested in Human Volunteers How are the Investigational Drugs Tested in Humans? How Does Testing Continue after a New Drug is Approved? Procedures Followed in Drug Design Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Principles of Drug Action Introduction Functional Group Review Stereochemistry Acid-Base Chemistry Biologically Significant Nitrogen-Containing Compounds Physicochemical Properties and Drug Action Bioisosteric Replacement Drug-Receptor Bonding G Protein-Coupled Receptors 49 Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Drug Metabolism and Prodrugs Drug Metabolism Phase I Reactions Phase II Reactions Prodrugs Introduction The Prodrug Concept Why Use Prodrugs? Characteristics of Prodrug Classification of Prodrugs Carrier-linked prodrugs Bioprecursor Prodrugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Computer-aided Drug Design Introduction Cadd Methodology Small Molecule-Based Drug Design Quantitative Structure-Activity Relationships Molecular descriptors Electronic parameters Hydrophobicity descriptors Steric descriptors Indicator or dummy parameters Molecular connectivity index Linear free energy relationship Topliss approach Pharmacophore-Based Drug Design Three-Dimensional QSAR Macromolecule-Based Drug Design Database Searching Method Ligand Building Method Substituent Constants Useful for Qsar Analysis Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions General Anaesthetics Introduction—Anaesthesia and its Stages Mechanism of Action Classification Inhalation Anaesthetics Liquid Anaesthetics Gaseous Anaesthetics Intravenous Anaesthetics Ultrashort Acting Barbiturates Arylcyclohexylamine Benzodiazepine Narcotic Analgesics Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Local Anaesthetics Introduction Ideal Properties of Local Anaesthetics Mechanism of Action Clinical Uses of Local Anaesthetics Classification of Local Anaesthetics Structures, Synthesis, and Structure-Activity Relationship of Benzoic Acid Derivatives Cocaine Hexylcaine Hydrochloride Meprylcaine and Isobucaine Hydrochloride Cyclomethycaine Sulphate Piperocaine Hydrochloride Structures, Synthesis, and SAR of P-Aminobenzoic Acid Derivatives Benzocaine Butamben Procaine Hydrochloride Chloroprocaine Tetracaine Butacaine Benoxinate Propoxycaine Proparacaine Hydrochloride Structure-activity relationships Structures, Synthesis, and SAR of Anilides Lidocaine Hydrochloride Prilocaine Hydrochloride Mepivacaine and Bupivacaine Hydrochloride Etidocaine Hydrochloride SAR of anilides Miscellaneous Phenacaine Hydrochloride Diperodon Pramoxine Hydrochloride Dyclonine Dibucaine Dimethisoquin Hydrochloride Newer Drugs Ropivacaine Levobupivacaine Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Sedatives, Hypnotics, and Anxiolytic Agents Introduction Classifi cation of Sedative and Hypnotics Barbiturates Benzodiazepines Benzodiazepine Antagonists Miscellaneous Anxiolytic Agents Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Anti-Epileptic Drugs Introduction: Epilepsy and Types of Seizures Classification Structural Requirements for Anticonvulsant Agents and Their Structure-Activity Relationship Hydantoins Oxazolidinediones Succinimides Benzodiazepines Gaba Analogues Miscellaneous Newer Anticonvulsants Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antipsychotic Agents Introduction Typical or Classical Antipsychotic Agents: Synthesis, Mechanism of Action, and SAR Atypical Antipsychotic Agents Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antidepressants Introduction Classification Mechanism of Action Side-Effects of Classical Antidepressants (Monoamino Oxidase MAO) Inhibitors Tricyclic Antidepressants Atypical Antidepressants Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Narcotic Analgesics Introduction Mechanism of Action Pharmacophore Requirement Clinical Uses Classification Morphine and its Derivatives Phenyl (Ethyl) Piperidines Diphenyl Heptanones Benzazocin (Benzomorphan) Derivatives Narcotic Antagonists Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antipyretics and Non-Steroidal Anti- Inflammatory Drugs Introduction Classification Biosynthesis of Eicosanoids Mechanism of Anti- Infl ammatory Action Side-Effects Salicylic Acid Derivatives P-Aminophenol Derivatives Pyrazolidinedione Derivatives Anthranilic Acid Derivatives Aryl Alkanoic Acid Derivatives Oxicams SAR (Structure Activity Relationship of Oxicams) Miscellaneous Drugs Anti-Gout Drugs Selective COX-2 Inhibitors Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Miscellaneous CNS Agents Anti-Parkinsonism Agents Muscle Relaxants Drugs for Alzheimer’s Disease Treatment CNS Stimulants Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antihistamines and Anti-Ulcer Agents Introduction H1 Receptor Antagonist H2 Receptor Antagonist Histamine H3 Receptors Histamine H4 Receptors Proton Pump Inhibitors Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Diuretics Introduction Uses Classification Osmotic Diuretics Carbonic Anhydrase Inhibitors Thiazide Diuretics Potassium-Sparing Diuretics Loop Diuretics Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution ot Multiple -Choice Questions Antihypertensive Agents Introduction Classification Peripheral Anti-Adrenergic Drugs Centrally Acting Antihypertensive Drugs Direct Vasodilators Ganglionic Blocking Agents β-Adrenergic Blockers Calcium Channel Blockers Angiotensin-Converting Enzyme (ACE) Inhibitors Angiotensin II Antagonists Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antiarrhythmic Drugs Introduction Classification Class II Agents Class III Agents Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antihyperlipidemic Agents Introduction Classification HMG-COA Reductase Inhibitors Aryloxyisobutyric Acid Derivatives Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antianginal Drugs Introduction Classification Nitrates/Nitrites β-Adrenergic Blockers Calcium Channel Blockers Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Insulin and Oral Hypoglycaemic Agents Introduction Insulin Oral Hypoglycaemic Agents Classifi cation Strategy For Controlling Hyperglycaemia Sulphonyl Ureas Biguanides Substituted Benzoic Acid Derivatives Thiazolidinediones Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Oral Anticoagulants Introduction Classification Coumarin Derivatives Indanedione Derivatives Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Adrenergic Drugs Introduction Sympathomimetic Drugs Sympathetic (Adrenergic) Blocking Agents (Sympatholytics) Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Cholinergic Drugs Introduction Cholinomimetics Anticholinesterases Cholinergic Blocking Agents Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Sulphonamides, Sulphones, and Dihydrofolate Reductase Inhibitors Sulphonamides Sulphones Dihydrofolate Reductase (DHFR) Inhibitors Newer Drug Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Quinolone Antibacterials Introduction Structures of Fluoroquinolones Mechanism of Action Uses Classification SAR of Quinolones Adverse Effects Synthesis of Fluoroquinolones Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antibiotics β-Lactam Antibiotics Tetracycline Antibiotics Macrolide Antibiotics Aminoglycoside Antibiotics Miscellaneous Antibiotics Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antitubercular Agents Introduction Mechanisms of Action Further Readings Multiple Choice Questions Questions Solution to Multiple- Choice Questions Antifungal Agents Introduction Classification Antifungal Antibiotics Azole Antifungals Pyrimidine Derivatives Miscellaneous Agents Newer Drugs Further Readings Multiple-Choice Questions Questions Solution to Multiple Choice Questions Antiviral Agents Anti-HIV Agents Anti-Herpes Simplex Virus Miscellaneous Agents Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Antiprotozoal Agents Introduction Antiamoebic Agents Antimalarial Agents Anthelmintics Miscellaneous Antiprotozoal Drugs Newer Drug Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Anticancer Agents Introduction Limitations of Therapy Classification Alkylating Agents Antimetabolites Anticancer Antibiotics Miscellaneous Drugs Anticancer Plant Products Hormones and Their Antagonists Miscellaneous Drugs Newer Drugs Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Prostaglandins Introduction Functions of Prostaglandins Biosynthesis of Prostaglandins Nomenclature Structures of Therapeutically useful Prostaglandins SAR of Prostaglandins Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Steroids Introduction Biosynthesis of Steroid Hormones Overall Mechanism of Action of Steroid Hormones Oestrogens Progestins Androgens Glucocorticoids Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Miscellaneous Agents Anti-Obesity Drugs PDE-5 Inhibitors for Male Erectile Dysfunction Anti-Migraine Drugs Anti-Asthmatics Thyroid and Anti-Thyroid Drugs Anti-Platelet Drugs Immunopharmacological Drugs Anti-Cough and Expectorants Diagnostic Agents Antiseptics and Disinfectants Some Important Antiseptics and Disinfectants Pharmaceutical Aid Vitamins Further Readings Multiple Choice Questions Questions Solution to Multiple Choice Questions Nomenclature of Medicinal Compounds Introduction General Rules Heterocyclic Compounds Examples Further Readings Questions Index