第二版前言
第一版前言
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 New Drug Development
1.3.1 General Process of New Drug Development
1.3.2 Precliblinical Development and Investigational New Drug Application
1.4 Problems
本章重点内容
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 Induced-Fit Theory
2.2.2 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
3 Enzymes and Enzyme Inhibition
3.1 Enzymes
3.1.1 Enzymes as Catalysts
3.1.2 Mechanism 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 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
References
本章重点内容
4 Drug Metabolism
4.1 Introduction
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
4.4 Problems
本章重点内容
5 Prodrugs and Drug Delivery System
5.1 Introduction
5.1.1 Utility of Prodrugs
5.1.2 Types of Prodrugs
5.2 Mechanism of Drug Activation
5.2.1 Carrier-Linked Prodrugs
……
6 Computer Aided Drug Design
7 Central Nervous System Drugs
8 Analgesics and Anesthetics
9 Drugs for Metabolic Syndrome Treatment
10 Agents for Gastrointestinal Diseases
11 Cardiovascular Agents
12 Anticancer Agents
13 Antivlral Agents
14 Antifungal Agents
15 Antibacterials
16 Antiparasitic
17 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs（NSAIDs）
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