藥物化學：英中雙語注解版(第二版)（簡體書）

《藥物化學(英中雙語注解版)(第2版)》對第一版進行了修訂，增減了相關內容，形式更緊湊，內容更精練。介紹藥物研發的基本理論與方法，以及目前新藥研究重點領域的藥物治療現狀、藥物的作用機理、構效關系等，并以代表性藥物作為案例進行講解。適合藥物化學專業的師生和專業技術人員使用。

第二版前言
第一版前言
1Drug Discovery，Design and Development
1.1Drug Discovery
1.1.1ADrug Discovery without a Lead
1.1.2Lead Discovery
1.2Lead Modification
1.2.1Identification of the ActivePart：The Pharmacophore
1.2.2Structure Modifications to Increase Potency and the The rapeutic Index
1.3New Drug Development
1.3.1General Process of New Drug Development
1.3.2Preclinical Development and Investigational New Drug Application
1.4Problems
本章重點內容
2Receptors
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
本章重點內容
3Enzymes 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
本章重點內容
4DrugMetabolism
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
本章重點內容
5Prodrugs and Drug Delivery System
5.1 Introduction
5.1.1 Utility of Prod_rugs
5.1.2 Types of Prodrugs
5.2 Mechanism of Drug Activation
5.2. 1 Carder-Linked Prodrugs
5.2.2 Bioprecursor Prodrugs
5.3 Problems
本章重點內容
6 Computer Aided Drug Design
6. 1 Introduction
6. 1.1 Molecular Mechanics and Empirical Force Field Methods
6. 1.2 Energy Minimization
6. 1.3 Conformational Analysis and Search
6. 2 Structure-Based Drug Design
6. 2. 1 Molecular Graphics-Based Drag Design
6. 2.2 Molecular Docking
6. 2. 3 De Novo Drugs Design
6.3 Ligand Based Drug Design
6.3.1 Quantitative Structure-Activity Relationships
6.3.2 Pharmacophore Modeling
6. 4 Problems
本章重點內容
7 Central Nervous System Drugs
7.1 Schizophrenia
7. 1.1 Introduction
7. 1.2 Stucture-activity Relationship of Tricyclic Anti-psychotics
7.1.3 Typical Drugs
7.1.4 Discovery and Development of New Antipsychotic Drags
7.2 Sedative-hypnotics
7.2. 1 Introduction
7.2. 2 Stucture-activity Relationship of Benzodiazepines
7.2.3 Typical Drugs
7.2.4 New Research Areas
7.3 Alzheimer's Disease
7.3.1 Introduction
7.3.2 Typical Drugs
7.3.3 New Research Areas
7.4 Problems
References
本章重點內容
8 Analgesics and Anesthetics
8. 1 Analgesics
8. 1.1 Introduction
8.1.2 Opioid Receptor
8. 1.3 Endogenous Opioid Peptides
8.1.4 Morphine and Related Opioids
8. 1.5 Synthetic Analgesics
8. 1.6 Unmet Medical Needs
8.1.7 New Research Areas
8.2 Anesthetics
8.2. 1 General Anesthetics
8.2. 2 Local Anesthetics
8.2.3 Unmet Medical Needs
8.3 Problems
本章重點內容
9 Drugs for Metabolic Syndrome Treatment
9. 1 . Obesity
9. 1.1 Current Treatment
9. 1.2 New Research Areas
9.2 Diabetes
9.2. 1 Current Treatment
9. 2.2 New Research Areas
9. 3 Problems
References
本章重點內容
10 Agents for Gastrointestinal Diseases
10. 1 Introduction
10. 1.1 The Function of Gastrointestinal Tract
10. 1.2 Historical Overview
10. 2 Gastric and Mucosal Ulceration
10. 2. 1 Overview
10. 2. 2 H2 Receptor Antagonists
10. 2.3 Proton Pump Inhibitors (PPIs)
10.2.4 New Research Areas
10. 3 Inflammatory Bowel Disease
10. 3 1 Overview
……
11Cardiovascular Agents
12Anticancer Agents
13Antiviral Agents
14Antifungal Agents
15Antibacterials
16Antiparasitic
17Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs(NSAIDs)

3. 4 Irreversible Enzyme Inhibitors
A competitive irreversible enzyme inhibitor, also known as an active-site directedirreversible inhibitor or an enzyme inactivator, is a compound whose structure is similar tothat of the substrate or product of the target enzyme and which generally forms a covalentbond to an active site residue. In the case of irreversible inhibition it is not necessary tosustain the inhibitor concentration to retain the enzyme-inhibitor interaction. Because this is anirreversible reaction, once the target enzyme has reacted with the irreversible inhibitor, thecomplex cannot dissociate, and, therefore, the enzyme remains inactive, even in the absenceof additional inhibitor. This effect could translate into the requirement for smaller and fewerdoses of the drug. Even though the target enzyme is destroyed by the irreversible inhibitor, itdoes not mean that only one dose of the drug would be sufficient to destroy the enzymepermanently. Yes, it destroys that copy of the enzyme permanently, but our genes areconstantly encoding more copies of proteins that diminish in concentration. As the enzymeloses activity, additional copies of the enzyme are synthesized, but this process can take hoursor even days. In some cases, however, particularly where genetic translation of the targetenzyme is slow, it may be safer to design reversible inhibitors whose effects can be controlledmore effectively by termination of their administration.
The term irreversible is a loose one; either a very stable covalent bond or a labile bondmay be formed between the drug and the enzyme active site. As pointed out earlier, some tight-binding reversible inhibitors also are functionally irreversible.