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内容大纲
本书是药物化学专业唯一一本英中双语教材。以英文编写,加以中文注释。
本书分为17章,前6章为总论部分,主要阐述药物研发的基本理论和基本方法,内容包括新药研究中先导化合物的发现和结构优化、药物与受体相互作用、酶及其抑制剂的基础理论和应用、药物代谢的基本概念、前药的设计及计算机辅助药物设计的基础知识。第7~17章为各论,按目前新药研究的重点领域分类,主要内容包括神经系统药物、镇痛及麻醉药、代谢综合征治疗药、胃肠道系统药物、心血管系统药物、抗肿瘤、抗病毒、抗真菌、抗感染及免疫抗炎药,重点讲解各类药物治疗现状、作用机制、结构与活性关系,代表性药物的合成路线设计、临床应用及药物代谢的相关知识。 -
作者介绍
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目录
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 Preclinical 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 Antiviral Agents
14 Antifungal Agents
15 Antibacterials
16 Antiparasitic
17 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs(NSAIDs)
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