前言 Chapter 1 Drug Discovery,Design and Development 1.1 Drug Discovery 1.1.1 A Drug Discovery Without a Lead 1.1.2 Lead Discovery 1.2 Lead Modification 1.2.1 Identification of the Active Part：The Pharmacophore 1.2.2 Structure Modifications to Increase Potency and the Therapeutic Index 1.3 Structure-Activity Relationships 1.4 Quantitative Structure…Activity Relationships 1.4.1 Methods Used to Correlate Physicochemical Parameters with Biological Activity：2D-QSAR 1.4.2 Computer-Based Methods of QSAR Related to Receptor Binding：3D-QSAR 1.4.3 Structure-Based Drug Design 1.5 New Drug Development 1.5.1 General Process of New Drug Development 1.5.2 Preclinical Development and Investigational New Drug Application 1.6 Problems 本章重点内容 Chapter 2 Receptors 2.1 Drug-Receptor Interactions 2.1.1 Interactions (Forces) Involved in the Drug-Receptor Complex 2.2 Theories for Drug-Receptor Interactions 2.2.1 Occupancy Theory 2.2.2 Rate Theory 2.2.3 Induced-Fit Theory 2.2.4 Macromolecular Perturbation Theory 2.2.5 Activation-Aggregation Theory 2.2.6 The Two-State (Multistate) Model of Receptor Activation 2.3 Topographical and Stereochemical Considerations 2.3.1 Spatial Arrangement of Atoms 2.3.2 Drug and Receptor Chirality 2.3.3 Geometric Isomers (Diastereomers) 2.3.4 Conformational Isomers 2.3.5 Ring Topology 2.4 Problems 本章重点内容 Chapter 3 Enzymes and Enzyme Inhibition 3.1 Enzymes 3.1.1 Enzymes as Catalysts 3.1.2 Mechanisms of Enzyme Catalysis 3.1.3 Coenzyme Catalysis 3.2 Enzyme Inhibition 3.2.1 Enzyme Inhibitors in Medicine 3.2.2 Design of Enzyme Inhibitors 3.3 Reversible Enzyme Inhibitors 3.3.1 Mechanism of Reversible Inhibition 3.3.2 Selected Examples of Competitive Reversible Inhibitor Drugs 3.3.3 Transition State Analogs 3.3.4 Multisubstrate Analogs 3.3.5 Slow，Tight-Binding Inhibitors 3.4 Irreversible Enzyme Inhibitors 3.4.1 Affinity Labeling Agents 3.4.2 Mechanism-Based Enzyme Inactivators 3.5 Problems 本章重点内容 Chapter 4 Drug Metabolism 4.1 Introduction 4.1.1 Definition of Drug Metabolism 4.1.2 Site of Drug Metabolism and First-Pass Effect 4.1.3 Purpose of Drug Metabolism Studies 4.1.4 Function of Drug Metabolism and Categories of Drug Metabolism Reaction 4.2 Phase I Transformations 4.2.1 Oxidative Reactions 4.2.2 Reductive Reactions 4.2.3 Carboxylation Reaction 4.2.4 Hydrolytic Reactions 4.3 Phase II Transformations：Conjugation Reactions 4.3.1 Introduction 4.3.2 Glucuronic Acid Conjugation 4.3.3 Sulfate Conjugation 4.3.4 Amino Acid Conjugation 4.3.5 Glutathione Conjugation 4.3.6 Acetyl Conjugation 4.3.7 Other Conjugation 4.4 Problems 本章重点内容 Chapter 5 Prodrugs and Drug Delivery Systems 5.1 Enzyme Activation of Drugs 5.1.1 Utility of Prodrugs 5.1.2 Types of Prodrugs 5.2 Mechanisms of Drug Activation 5.2.1 Carrier-Linked Prodrugs 5.2.2 Bioprecursor Prodrugs 5.3 Problems 本章重点内容 Chapter 6 Central Nervous System Drugs 6.1 Schizophrenia 6.1.1 Introduction 6.1.2 Disease Basis 6.1.3 Current Treatment 6.1.4 Stucture-activity Relationship of Tricyclic Anti-psychotics 6.1.5 Unmet Medical Needs 6.1.6 New Research Areas 6.2 Affective Disorders：Depression and Bipolar Disease 6.2.1 Introduction 6.2.2 Disease Basis 6.2.3 Current Treatment 6.2.4 Stucture-activity Relationship of Tricyclic antidepressants 6.2.5 Unmet Medical Needs 6.2.6 New Research Areas 6.3 Anxiety 6.3.1 Introduction 6.3.2 Disease Basis 6.3.3 Current Treatments 6.3.4 Stucture-activity Relationship of Benzodiazepines 6.3.5 New Research Areas 6.4 Sleep Disorders 6.4.1 Introduction 6.4.2 Disease Basis 6.4.3 Current Treatment 6.4.4 Unmet Medical Needs 6.4.5 New Research Areas 6.5 Epilepsy 6.5.1 Introduction 6.5.2 Disease Basis 6.5.3 Current Treatment 6.5.4 Stucture-activity Relationship on homotypical drugs of Barbiturates 6.5.5 Unmet Medical Needs 6.5.6 New Research Areas 6.6 Addiction 6.6.1 Introduction 6.6.2 Disease Basis 6.6.3 Current Treatment 6.6.4 Unmet Medical Needs 6.6.5 New Research Areas 6.7 Neurodegeneration 6.7.1 Overview 6.7.2 Alzheimer's Disease 6.7.3 Parkinson's Disease 6.7.4 Future Aspects 6.8 Problems References 本章重点内容 Chapter 7 Analgesics and Anesthetics 7.1 Analgesics 7.1.1 Introduction 7.1.2 Opioid Receptor 7.1.3 Endogenous Opioid Peptides 7.1.4 Morphine and Related Opioids 7.1.5 Synthesis Analgesics 7.1.6 Opioid Agonist/Antagonists and Partial Agonists 7.1.7 Opioid Antagonists 7.1.8 Structure-Activity Relationships 7.1.9 Unmet Medical Needs 7.1.10 New Research Areas 7.2 Anesthetics 7.2.1 General Anesthetics 7.2.2 Local Anesthetics 7.2.3 Unmet Medical Needs 7.2.4 New Research Areas 7.3 Problem 本章重点内容 Chapter 8 Drugs for Metabolic Syndrome Treatment 8.1 Introduction 8.1.1 Definition of Metabolic Syndrome(Mats) 8.1.2 Management of the Metabolic Syndrome 8.2 Obesity/Disorders of Energy 8.2.1 Disease State 8.2.2 Disease Basis 8.2.3 Current Treatment 8.2.4 Unmet Medical Needs 8.2.5 New Research Areas 8.3 Diabetes 8.3.1 Introduction 8.3.2 Disease Basis 8.3.3 Current Treatment 8.3.4 Unmet Medical Needs 8.3.5 New Research Areas 8.4 Problems References 本章重点内容 Chapter 9 Agents for Gastrointestinal Diseases 9.1 Introduction 9.1.1 The Function of Gastrointestinal Tract 9.1.2 Historical Overview 9.2 Gastric and Mucosal Ulceration 9.2.1 Overview 9.2.2 Disease Basis 9.2.3 Current Treatment 9.2.4 Unmet Medical Needs 9.2.5 New Research Areas 9.3 Inflammatory Bowel Disease 9.3.1 Overview 9.3.2 Disease Basis 9.3.3 Current Treatment 9.3.4 Unmet Medical Needs 9.3.5 New research Areas 9.4 Emesis/Prokinetic Agents 9.4.1 Overview 9.4.2 Disease Basis 9.4.3 Current Treatment 9.4.4 Unmet Medical Needs 9.4.5 New research Areas 9.5 Problems References 本章重点内容 Chapter 10 Cardiovascular Agents 10.1 Introduction 10.2 Hypertension 10.2.1 Disease Basis 10.2.2 Current Antihypertensive Agents 10.2.3 Unmet Medical Needs 10.2.4 New Research Areas 10.3 Cardiac Arrhythmias 10.3.1 Disease Basis 10.3.2 Current Anti-arrhythmic Agents 10.3.3 Unmet Medical Needs 10.3.4 New Research Areas 10.4 Congestive Heart Failure 10.4.1 Disease Basis 10.4.2 Current Cardiac Agents 10.5 Angina 10.5.1 Disease Basis 10.5.2 Current Anti-anginal Agents 10.6 Hyperlipidemias 10.6.1 Disease Basis 10.6.2 Anti-hyperlipidemic Agents 10.7 Problems References 选读资料 本章重点内容 Chapter 11 Anticancer Agents 11.1 Introduction 11.2 Alkylating and Platinum Anticancer Agents 11.2.1 Current Treatments 11.2.2 Platinum Complexes 11.3 Deoxyribonucleic Acid Topoisomerase Inhibitors 11.3.1 TopoisomeraseⅠInhibitors Camptothecin and Analogs 11.3.2 Topoisomerase II Inhibitors 11.4 Antimetabolites 11.4.1 Current Treatment 11.5 Microtubule Targeting Agents 11.5.1 Inhibitors of Microtubule Assembly 11.5.2 Microtubule Stabilizers 11.6 Unmet Medical Needs and New Research Areas 11.6.1 Tyrosine Kinase and Inhibitors 11.6.2 Multi-targeted Kinase Inhibitors 11.6.3 Histone Deacetylase Inhibitors 11.6.4 Proteasome Inhibitors 11.6.5 Other New Research Areas 11.7 Problems References 本章重点内容 Chapter 12 Antiviral 12.1 Antivirals for Herpesviruses 12.1.1 Introduction 12.1.3 Current Treatment 12.1.4 Structure-activity Relationship 12.1.5 Unmet Medical Needs 12.1.6 New Research Areas 12.2 Antivirals for Human Immunodeficiency Virus 12.2.1 Introduction 12.2.2 Disease Basis 12.2.3 Current Treatment 12.2.4 Structure-activity Relationship 12.2.5 Unmet Medical Needs 12.2.6 New Research Areas 12.3 Antivirals for Influenza Virus 12.3.1 Introduction 12.3.2 Disease Basis 12.3.3 Current Treatment 12.3.4 Structure-activity Relationship 12.3.5 Unmet Medical Needs 12.3.6 New Research Areas 12.4 Problems 选读资料 本章重点内容 Chapter 13 Antifungal Agents 13.1 Introduction 13.1.1 General Classification and Structure of Medically Important Fungi 13.1.2 Human Pathogenic Fungi and Disease States 13.2 Current Antifungal Agents 13.2.1 General 13.2.2 The Mechanism of Action 13.3 Typical Antifungal Drugs in Clinical Use 13.3.1 Amphotericin B 13.3.2 Azoles 13.3.3 Allylamines 13.4 New Research Areas 13.4.1 Overview 13.4.2 Isoleucyl-tRNA Synthetase Inhibitors (ITRS) 13.4.3 Sphingolipid Biosynthesis Inhibitors 13.5 Problems 本章重点内容 Chapter 14 Antibacterials 14.1 Introduction 14.2 β-lactam 14.2.1 History and Overview 14.2.2 Mode of Action 14.2.3 Mechanisms of Resistance 14.2.4 Major Drug Classes 14.3 Macrolide 14.3.1 Introduction 14.3.2 Mechanism of Action 14.3.3 Major Classes of Macrolides 14.4 Tetracyclines 14.4.1 Introduction 14.4.2 SAR of Tetracyclines 14.4.3 Mechanism of Action 14.4.4 Major Classes of Tetracyclines 14.4.5 Antibacterial Resistance to the Tetracyclines 14.5 Quinolones 14.5.1 Overview of Quinolones 14.5.2 Mechanism of Antibacterial Action 14.5.3 SAR and STR of Quinolones 14.5.4 Antibacterial Resistance Mechanisms 14.5.5 Synthesis of Quinolones 14.6 Oxazolidinone 14.6.1 Introduction 14.6.2 SAR Leading to DuP-721 and DuP-105 14.6.3 SAR Leading to Eperezolid and Linezolid 14.6.4 Synthesis of Linezolid 14.6.5 Mode of Action 14.7 Aminoglycosides，glycopeptides，and others 14.7.1 Vancomycin 14.7.2 Aminoglycosides 14.7.3 Dapotamycin 14.8 Antimycobacterium Agents 14.8.1 Introduction 14.8.2 Rifamycin 14.8.3 Isoniazid 14.9 Resistance and Challenge[3] 14.10 Problems References 本章重点内容 Chapter 15 Antiparasitics 15.1 Introduction 15.2 Representative Diseases 15.2.1 African Trypanosomiasis 15.2.2 Chagas disease 15.2.3 Leishmaniasis 15.2.4 Malaria 15.3 Antimalarias 15.3.1 Quinolines 15.3.2 Artemisinin and its analogs 15.4 Problems References 本章重点内容 Chapter 16 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs (NSAIDs) 16.1 Introduction 16.1.1 Arthritis 16.1.2 Other Inflammatory and Immunological Diseases 16.2 Disease Basis 16.2.1 Arachidonic Acid Cascade 16.2.2 Phospholipase A2 (PLA2) 16.2.3 Cyclooxygenase (COX) 16.2.4 Lipoxygenase (LOX) 16.3 Current Treatment for Arthritis 16.3.1 Steroids (Brief Introduction) 16.3.2 Nonsteroidal Anti-inflammatory Drugs (NSAIDs) 16.4 New Research Areas 16.4.1 Disease-modifying Anti-rheumatic Drugs 16.4.2 Structure-modifying Anti-inflammatory Drugs 16.5 Conclusions and Future Directions 16.6 Problems References 本章重点内容 索引
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