药物化学 英中双语注解版2025|PDF|Epub|mobi|kindle电子书版本百度云盘下载

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1 Drug Discovery,Design and Development1

1.1 Drug Discovery1

1.1.1 A Drug Discovery without a Lead2

1.1.2 Lead Discovery4

1.2 Lead Modification8

1.2.1 Identification of the Active Part:The Pharmacophore8

1.2.2 Structure Modifications to Increase Potency and the Therapeutic Index11

1.3 New Drug Development19

1.3.1 General Process of New Drug Development19

1.3.2 Preclinical Development and Investigational New Drug Application21

1.4 Problems22

本章重点内容23

2 Receptors24

2.1 Drug-Receptor Interactions24

2.1.1 Interactions(Forces)Involved in the Drug-Receptor Complex24

2.2 Theories for Drug-Receptor Interactions32

2.2.1 Induced-Fit Theory32

2.2.2 The Two-State(Multistate)Model of Receptor Activation33

2.3 Topographical and Stereochemical Considerations35

2.3.1 Spatial Arrangement of Atoms35

2.3.2 Drug and Receptor Chirality36

2.3.3 Geometric Isomers(Diastereomers)41

2.3.4 Conformational Isomers41

2.3.5 Ring Topology45

2.4 Problems46

本章重点内容48

3 Enzymes and Enzyme Inhibition51

3.1 Enzymes51

3.1.1 Enzymes as Catalysts51

3.1.2 Mechanism of Enzyme Catalysis55

3.1.3 Coenzyme Catalysis58

3.2 Enzyme Inhibition61

3.2.1 Enzyme Inhibitors in Medicine61

3.2.2 Design of Enzyme Inhibitors62

3.3 Reversible Enzyme Inhibitors64

3.3.1 Mechanism of Reversible Inhibition64

3.3.2 Selected Examples of Competitive Reversible Inhibitor Drugs66

3.3.3 Transition State Analogs67

3.3.4 Slow,Tight-Binding Inhibitors68

3.4 Irreversible Enzyme Inhibitors70

3.4.1 Affinity Labeling Agents71

3.4.2 Mechanism-Based Enzyme Inactivators73

3.5 Problems76

References77

本章重点内容78

4 Drug Metabolism80

4.1 Introduction80

4.2 Phase Ⅰ Transformations81

4.2.1 Oxidative Reactions81

4.2.2 Reductive Reactions93

4.2.3 Carboxylation Reaction97

4.2.4 Hydrolytic Reactions98

4.3 Phase Ⅱ Transformations:Conjugation Reactions99

4.3.1 Introduction99

4.3.2 Glucuronic Acid Conjugation100

4.3.3 Sulfate Conjugation103

4.3.4 Amino Acid Conjugation104

4.3.5 Glutathione Conjugation105

4.3.6 Acetyl Conjugation107

4.4 Problems109

本章重点内容111

5 Prodrugs and Drug Delivery System113

5.1 Introduction113

5.1.1 Utility of Prodrugs113

5.1.2 Types of Prodrugs115

5.2 Mechanism of Drug Activation116

5.2.1 Carrier-Linked Prodrugs116

5.2.2 Bioprecursor Prodrugs129

5.3 Problems137

本章重点内容138

6 Computer Aided Drug Design139

6.1 Introduction139

6.1.1 Molecular Mechanics and Empirical Force Field Methods140

6.1.2 Energy Minimization142

6.1.3 Conformational Analysis and Search142

6.2 Structure-Based Drug Design142

6.2.1 Molecular Graphics-Based Drug Design143

6.2.2 Molecular Docking145

6.2.3 De Novo Drugs Design146

6.3 Ligand Based Drug Design149

6.3.1 Quantitative Structure-Activity Relationships149

6.3.2 Pharmacophore Modeling154

6.4 Problems159

本章重点内容160

7 Central Nervous System Drugs161

7.1 Schizophrenia161

7.1.1 Introduction161

7.1.2 Stucture-activity Relationship of Tricyclic Anti-psychotics165

7.1.3 Typical Drugs166

7.1.4 Discovery and Development of New Antipsychotic Drugs168

7.2 Sedative-hypnotics171

7.2.1 Introduction171

7.2.2 Stucture-activity Relationship of Benzodiazepines175

7.2.3 Typical Drugs177

7.2.4 New Research Areas181

7.3 Alzheimer's Disease183

7.3.1 Introduction183

7.3.2 Typical Drugs186

7.3.3 New Research Areas191

7.4 Problems195

References195

本章重点内容197

8 Analgesics and Anesthetics199

8.1 Analgesics199

8.1.1 Introduction199

8.1.2 Opioid Receptor200

8.1.3 Endogenous Opioid Peptides200

8.1.4 Morphine and Related Opioids201

8.1.5 Synthetic Analgesics204

8.1.6 Unmet Medical Needs211

8.1.7 New Research Areas212

8.2 Anesthetics213

8.2.1 General Anesthetics213

8.2.2 Local Anesthetics217

8.2.3 Unmet Medical Needs222

8.3 Problems224

本章重点内容225

9 Drugs for Metabolic Syndrome Treatment227

9.1 Obesity227

9.1.1 Current Treatment227

9.1.2 New Research Areas228

9.2 Diabetes228

9.2.1 Current Treatment230

9.2.2 New Research Areas242

9.3 Problems246

References247

本章重点内容248

10 Agents for Gastrointestinal Diseases250

10.1 Introduction250

10.1.1 The Function of Gastrointestinal Tract250

10.1.2 Historical Overview250

10.2 Gastric and Mucosal Ulceration252

10.2.1 Overview252

10.2.2 H2 Receptor Antagonists254

10.2.3 Proton Pump Inhibitors(PPIs)257

10.2.4 New Research Areas260

10.3 Inflammatory Bowel Disease260

10.3.1 Overview260

10.3.2 New Research Areas262

10.4 Emesis/Prokinetic Agents264

10.4.1 Overview264

10.4.2 New Research Areas270

10.5 Problems271

References271

本章重点内容272

11 Cardiovascular Agents274

11.1 Introduction274

11.2 Hypertension274

11.2.1 Introduction274

11.2.2 Antihypertensive Agents275

11.2.3 New Research Areas296

11.3 Cardiac Arrhythmias297

11.3.1 Introduction297

11.3.2 Antiarrhythmic Agents298

11.3.3 New Research Areas303

11.4 Congestive Heart Failure303

11.4.1 Introduction303

11.4.2 Cardiac Agents304

11.5 Angina306

11.5.1 Introduction306

11.5.2 Antianginal Agents306

11.6 Hyperlipidemias307

11.6.1 Introduction307

11.6.2 Antihyperlipidemic Agents308

References314

选读资料315

本章重点内容316

12 Anticancer Agents318

12.1 Introduction318

12.2 Current Anticancer Agents318

12.2.1 Alkylating and Platinum Anticancer Agents318

12.2.2 Deoxyribonucleic Acid Topoisomerase Inhibitors329

12.2.3 Antimetabolic Agents333

12.2.4 Microtubule Targeting Agents341

12.3 New Research Areas345

12.3.1 Tyrosine Kinase and Inhibitors346

12.3.2 Histone Deacetylase Inhibitors349

12.3.3 Proteasome Inhibitors351

12.3.4 Other New Research Areas of Anticancer Drugs351

12.4 Problems352

References352

本章重点内容353

13 Antiviral Agents356

13.1 Overview of Virus Infections and Antiviral Agents356

13.2 Antivirals for Herpesviruses357

13.2.1 Introduction357

13.2.2 Current Antiherpes Drugs357

13.2.3 Structure-activity Relationship359

13.2.4 New Research Areas362

13.3 Antivirals for Human Immunodeficiency Virus362

13.3.1 Introduction362

13.3.2 HIV Reverse Transcriptase Inhibitors364

13.3.3 HIV Protease Inhibitors366

13.3.4 New Research Areas371

13.4 Antivirals for Influenza Virus373

13.4.1 Introduction373

13.4.2 M2 Ion Channel Inhibitors373

13.4.3 Neuraminidase Inhibitors375

13.4.4 New Research Areas379

13.5 Problems379

References380

本章重点内容381

14 Antifungal Agents383

14.1 Introduction383

14.1.1 Fungi383

14.1.2 Fungal infections384

14.2 Current Antifungal Agents385

14.2.1 General385

14.2.2 The Mechanism of Action of Major Antifungal Agents386

14.3 Typical Antifungal Drugs in Clinical Use390

14.3.1 Azoles Antifungal Drugs390

14.3.2 Allyamines398

14.4 Antifungal Drug Discovery and Development:New Modes of Action400

14.4.1 Overview400

14.4.2 Emerging Targets for The Development of Novel Antifungal Therapeutics401

14.5 Problems403

本章重点内容404

15 Antibacterials406

15.1 Introduction406

15.2 β-lactam408

15.2.1 History and Overview408

15.2.2 Mode of Action410

15.2.3 Mechanisms of Resistance413

15.2.4 Major Drug Classes414

15.3 Macrolide419

15.3.1 Introduction419

15.3.2 Major Classes of Macrolides420

15.4 Tetracyclines425

15.4.1 Introduction425

15.4.2 SAR of Tetracyclines425

15.4.3 Mechanism of Action426

15.5 Aminoglycosides427

15.6 Quinolones430

15.6.1 Overview of Quinolones430

15.6.2 Mechanism of Antibacterial Action432

15.6.3 SAR and STR of Quinolones432

15.6.4 Antibacterial Resistance Mechanisms433

15.7 Antimycobacterial Agents435

15.7.1 Introduction435

15.7.2 Rifamycin436

15.7.3 Isoniazid436

15.8 Resistance and Challenge438

15.9 Problems439

本章重点内容440

16 Antiparasitic443

16.1 Introduction443

16.2 Representative Diseases445

16.2.1 Chagas Disease445

16.2.2 Leishmaniasis445

16.2.3 Malaria446

16.3 Antimalarias447

16.3.1 Quinolines449

16.3.2 Artemisinin and its Analogs453

16.4 Questions457

References457

本章重点内容458

17 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs(NSAIDs)460

17.1 Introduction[1-3]460

17.1.1 Arthritis461

17.1.2 Arachidonic Acid Cascade461

17.1.3 Phospholipase A2(PLA2)464

17.1.4 Cyclooxygenase(COX)465

17.1.5 Lipoxygenase(LOX)466

17.2 Current Treatment for Arthritis466

17.2.1 Steroids(brief introduction)466

17.2.2 Nonsteroidal Anti-inflammatory Drugs(NSAIDs)466

17.3 Typical Nonsteroidal Anti-inflammatory Drugs in Clinical Use477

17.4 New Research Areas487

17.4.1 Dual COX-LOX Inhibitors487

17.4.2 Disease-modifying Anti-rheumatic Drugs487

17.4.3 Structure-modifying Anti-inflammatory Drugs488

17.5 Conclusions and Future Directions490

17.6 Problems490

References491

本章重点内容492