药物化学 英汉双语教材 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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Chapter 1　Drug Discovery,Design and Development1

1.1 Drug Discovery1

1.1.1 ADrug Discovery Without a Lead2

1.1.2 Lead Discovery5

1.2 Lead Modification9

1.2.1 Identification of the Active Part:The Pharmacophore9

1.2.2 Structure Modifications to Increase Potency and the Therapeutic Index12

1.3 Structure-Activity Relationships21

1.4 Quantitative Structure-Activity Relationships23

1.4.1 Methods Used to Correlate Physicochemical Parameters with Biological Activity:2D-QSAR24

1.4.2 Computer-Based Methods of QSAR Related to Receptor Binding:3D-QSAR26

1.4.3 Structure-Based Drug Design29

1.5 New Drug Development36

1.5.1 General Process of New Drug Development36

1.5.2 Preclinical Development and Investigational New Drug Application38

1.6 Problems39

本章重点内容40

Chapter 2 Receptors42

2.1 Drug-Receptor Interactions42

2.1.1 Interactions(Forces)Involved in the Drug-Receptor Complex42

2.2 Theories for Drug-Receptor Interactions51

2.2.1 Occupancy Theory51

2.2.2 Rate Theory53

2.2.3 Induced-Fit Theory53

2.2.4 Macromolecular Perturbation Theory54

2.2.5 Activation-Aggregation Theory55

2.2.6 The Two-State(Multistate)Model of Receptor Activation55

2.3 Topographical and Stereochemical Considerations57

2.3.1 Spatial Arrangement of Atoms57

2.3.2 Drug and Receptor Chirality58

2.3.3 Geometric Isomers(Diastereomers)69

2.3.4 Conformational Isomers70

2.3.5 Ring Topology76

2.4 Problems77

本章重点内容80

Chapter 3 Enzymes and Enzyme Inhibition83

3.1 Enzymes83

3.1.1 Enzymes as Catalysts83

3.1.2 Mechanisms of Enzyme Catalysis88

3.1.3 Coenzyme Catalysis92

3.2 Enzyme Inhibition95

3.2.1 Enzyme Inhibitors in Medicine95

3.2 2 Design of Enzyme Inhibitors96

3.3 Reversible Enzyme Inhibitors99

3.3.1 Mechanism of Reversible Inhibition99

3.3.2 Selected Examples of Competitive Reversible Inhibitor Drugs101

3.3.3 Transition State Analogs103

3.3.4 Multisubstrate Analogs105

3.3.5 Slow,Tight-Binding Inhibitors106

3.4 Irreversible Enzyme Inhibitors108

3.4.1 Affinity Labeling Agents108

3.4.2 Mechanism-Based Enzyme Inactivators111

3.5 Problems114

本章重点内容116

Chapter 4 Drug Metabolism118

4.1 Introduction118

4.1.1 Definition of Drug Metabolism118

4.1.2 Site of Drug Metabolism and First-Pass Effect118

4.1.3 Purpose of Drug Metabolism Studies119

4.1.4 Function of Drug Metabolism and Categories of Drug Metabolism Reaction120

4.2 Phase Ⅰ Transformations121

4.2.1 Oxidative Reactions121

4.2.2 Reductive Reactions135

4.2.3 Carboxylation Reaction139

4.2.4 Hydrolytic Reactions140

4.3 Phase Ⅱ Transformations:Conjugation Reactions141

4.3.1 Introduction141

4.3.2 Glucuronic Acid Conjugation143

4.3.3 Sulfate Conjugation145

4.3.4 Amino Acid Conjugation146

4.3.5 Glutathione Conjugation148

4.3.6 Acetyl Conjugation150

4.3.7 Other Conjugation152

4.4 Problems153

本章重点内容155

Chapter 5 Prodrugs and Drug Delivery Systems157

5.1 Enzyme Activation of Drugs157

5.1.1 Utility of Prodrugs157

5.1.2 Types of Prodrugs159

5.2 Mechanisms of Drug Activation160

5.2.1 Carrier-Linked Prodrugs160

5.2.2 Bioprecursor Prodrugs177

5.3 Problems189

本章重点内容190

Chapter 6 Central Nervous System Drugs191

6.1 Schizophrenia191

6.1.1 Introduction191

6.1.2 Disease Basis191

6.1.3 Current Treatment193

6.1.4 Stucture-activity Relationship of Tricyclic Anti-psychotics197

6.1.5 Unmet Medical Needs201

6.1.6 New Research Areas202

6.2 Affective Disorders:Depression and Bipolar Disease203

6.2.1 Introduction203

6.2 2 Disease Basis204

6.2.3 Current Treatment204

6.2.4 Stucture-activity Relationship of Tricyclic antidepressants209

6.2.5 Unmet Medical Needs211

6.2.6 New Research Areas211

6.3 Anxiety212

6.3.1 Introduction212

6.3.2 Disease Basis213

6.3.3 Current Treatments213

6.3.4 Stucture-activity Relationship of Benzodiazepines216

6.3.5 New Research Areas218

6.4 Sleep Disorders218

6.4.1 Introduction218

6.4.2 Disease Basis219

6.4.3 Current Treatment219

6.4.4 Unmet Medical Needs225

6.4.5 New Research Areas225

6.5 Epilepsy225

6.5.1 Introduction225

6.5.2 Disease Basis226

6.5.3 Current Treatment226

6.5.4 Stucture-activity Relationship on homotypical drugs of Barbiturates228

6.5.5 Unmet Medical Needs229

6.5.6 New Research Areas230

6.6 Addiction231

6.6.1 Introduction231

6.6.2 Disease Basis233

6.6.3 Current Treatment234

6.6.4 Unmet Medical Needs236

6.6.5 New Research Areas236

6.7 Neurodegeneration236

6.7.1 Overview236

6.7.2 Alzheimer's Disease238

6.7.3 Parkinson's Disease248

6.7.4 Future Aspects253

6.8 Problems254

References254

本章重点内容255

Chapter 7 Analgesics and Anesthetics258

7.1 Analgesics258

7.1.1 Introduction258

7.1.2 Opioid Receptor260

7.1.3 Endogenous Opioid Peptides260

7.1.4 Morphine and Related Opioids261

7.1.5 Synthesis Analgesics265

7.1.6 Opioid Agonist/Antagonists and Partial Agonists270

7.1.7 Opioid Antagonists270

7.1.8 Structure-Activity Relationships271

7.1.9 Unmet Medical Needs273

7.1.10 New Research Areas273

7.2 Anesthetics274

7.2.1 General Anesthetics274

7.2.2 Local Anesthetics279

7.2.3 Unmet Medical Needs287

7.2.4 New Research Areas288

7.3 Problem289

本章重点内容290

Chapter 8 Drugs for Metabolic Syndrome Treatment292

8.1 Introduction292

8.1.1 Definition of Metabolic Syndrome(Mats)292

8.1.2 Management of the Metabolic Syndrome292

8.2 Obesity/Disorders of Energy293

8.2.1 Disease State293

8.2.2 Disease Basis294

8.2.3 Current Treatment294

8.2.4 Unmet Medical Needs299

8.2.5 New Research Areas302

8.3 Diabetes308

8.3.1 Introduction308

8.3.2 Disease Basis309

8.3.3 Current Treatment313

8.3.4 Unmet Medical Needs327

8.3.5 New Research Areas328

8.4 Problems332

References332

本章重点内容333

Chapter 9 Agents for Gastrointestinal Diseases335

9.1 Introduction335

9.1.1 The Function of Gastrointestinal Tract335

9.1.2 Historical Overview335

9.2 Gastric and Mucosal Ulceration338

9.2.1 Overview338

9.2.2 Disease Basis338

9.2.3 Current Treatment339

9.2.4 Unmet Medical Needs348

9.2.5 New Research Areas349

9.3 Inflammatory Bowel Disease349

9.3.1 Overview349

9.3.2 Disease Basis350

9.3.3 Current Treatment351

9.3.4 Unmet Medical Needs355

9.3.5 New research Areas355

9.4 Emesis/Prokinetic Agents358

9.4.1 Overview358

9.4.2 Disease Basis358

9.4.3　Current Treatment360

9.4.4　Unmet Medical Needs368

9.4.5　New research Areas368

9.5　Problems369

References369

本章重点内容370

Chapter 10　Cardiovascular Agents372

10.1　Introduction372

10.2　Hypertension372

10.2.1　Disease Basis372

10.2.2　Current Antihypertensive Agents374

10.2.3　Unmet Medical Needs396

10.2.4　New Research Areas397

10.3　Cardiac Arrhythmias397

10.3.1　Disease Basis397

10.3.2　Current Anti-arrhythmic Agents398

10.3.3　Unmet Medical Needs406

10.3.4　New Research Areas406

10.4　Congestive Heart Failure407

10.4.1　Disease Basis407

10.4.2　Current Cardiac Agents407

10.5　Angina411

10.5.1　Disease Basis411

10.5.2　Current Anti-anginal Agents411

10.6　Hyperlipidemias413

10.6.1　Disease Basis413

10.6.2　Anti-hyperlipidemic Agents415

10.7　Problems424

References424

选读资料425

本章重点内容426

Chapter 11　Anticancer Agents429

11.1　Introduction429

11.2　Alkylating and Platinum Anticancer Agents429

11.2.1　Current Treatments430

11.2.2　Platinum Complexes439

11.3　Deoxyribonucleic Acid Topoisomerase Inhibitors441

11.3.1　Topoisomerase Ⅰ Inhibitors Camptothecin and Analogs442

11.3.2　Topoisomerase Ⅱ Inhibitors443

11.4 Antimetabolites449

11.4.1 Current Treatment449

11.5 Microtubule Targeting Agents457

11.5.1 Inhibitors of Microtubule Assembly458

11.5.2 Microtubule Stabilizers460

11.6 Unmet Medical Needs and New Research Areas462

11.6.1 Tyrosine Kinase and Inhibitors463

11.6.2 Multi-targeted Kinase Inhibitors465

11.6.3 Histone Deacetylase Inhibitors466

11.6.4 Proteasome Inhibitors467

11.6.5 Other New Research Areas468

11.7 Problems469

References469

本章重点内容470

Chapter 12 Antiviral472

12.1 Antivirals for Herpesviruses472

12.1.1 Introduction472

12.1.2 Disease Basis473

12.1.3 Current Treatment473

12.1.4 Structure-activity Relationship477

12.1.5 Unmet Medical Needs480

12.1.6 New Research Areas480

12.2 Antivirals for Human Immunodeficiency Virus481

12.2.1 Introduction481

12.2.2 Disease Basis481

12.2.3 Current Treatment482

12.2.4 Structure-activity Relationship488

12.2.5 Unmet Medical Needs492

12.2.6 New Research Areas493

12.3 Antivirals for Influenza Virus496

12.3.1 Introduction496

12.3.2 Disease Basis496

12.3.3 Current Treatment497

12.3.4 Structure-activity Relationship500

12.3.5 Unmet Medical Needs504

12.3.6 New Research Areas504

12.4 Problems505

选读资料505

本章重点内容506

Chapter 13 Antifungal Agents508

13.1 Introduction508

13.1.1 General Classification and Structure of Medically Important Fungi508

13.1.2 Human Pathogenic Fungi and Disease States509

13.2 Current Antifungal Agents511

13.2.1 General511

13.2.2 The Mechanism of Action512

13.3 Typical Antifungal Drugs in Clinical Use513

13.3.1 Amphotericin B513

13.3.2 Azoles516

13.3.3 Allylamines522

13.4 New Research Areas525

13.4.1 Overview525

13.4.2 Isoleucyl-tRNA Synthetase Inhibitors(ITRS)525

13.4.3 Sphingolipid Biosynthesis Inhibitors526

13.5 Problems527

本章重点内容528

Chapter 14 Antibacterials529

14.1 Introduction529

14.2 β-lactam532

14.2.1 History and Overview532

14.2.2 Mode of Action534

14.2.3 Mechanisms of Resistance537

14.2.4 Major Drug Classes539

14.3 Macrolide547

14.3.1 Introduction547

14.3.2 Mechanism of Action548

14.3.3 Major Classes of Macrolides551

14.4 Tetracyclines557

14.4.1 Introduction557

14.4.2 SAR of Tetracyclines558

14.4.3 Mechanism of Action559

14.4.4 Major Classes of Tetracyclines561

14.4.5 Antibacterial Resistance to the Tetracyclines563

14.5 Quinolones565

14.5.1 Overview of Quinolones565

14.5.2 Mechanism of Antibacterial Action567

14.5.3 SAR and STR of Quinolones568

14.5.4 Antibacterial Resistance Mechanisms568

14.5.5 Synthesis of Quinolones568

14.6 Oxazolidinone571

14.6.1 Introduction571

14.6.2 SAR Leading to DuP-721 and DuP-105572

14.6.3 SAR Leading to Eperezolid and Linezolid572

14.6.4 Synthesis of Linezolid574

14.6.5 Mode of Action575

14.7 Aminoglycosides,glycopeptides,and others575

14.7.1 Vancomycin575

14.7.2 Aminoglycosides576

14.7.3 Dapotamycin578

14.8 Antimycobacterium Agents579

14.8.1 Introduction579

14.8.2 Rifamycin581

14.8.3 Isoniazid581

14.9 Resistance and Challenge[3]583

14.10 Problems585

References585

本章重点内容586

Chapter 15 Antiparasitics589

15.1 Introduction589

15.2 Representative Diseases590

15.2.1 African Trypanosomiasis590

15.2.2 Chagas disease591

15.2.3 Leishmaniasis592

15.2.4 Malaria593

15.3 Antimalarias594

15.3.1 Quinolines596

15.3.2 Artemisinin and its analogs600

15.4 Problems604

References605

本章重点内容606

Chapter 16 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs(NSAIDs)608

16.1 Introduction608

16.1.1 Arthritis609

16.1.2 Other Inflammatory and Immunological Diseases612

16.2 Disease Basis614

16.2.1 Arachidonic Acid Cascade614

16.2.2 Phospholipase A2(PLA2)616

16.2.3 Cyclooxygenase(COX)618

16.2.4 Lipoxygenase(LOX)619

16.3 Current Treatment for Arthritis620

16.3.1 Steroids(Brief Introduction)620

16.3.2 Nonsteroidal Anti-inflammatory Drugs(NSAIDs)622

16.4 New Research Areas644

16.4.1 Disease-modifying Anti-rheumatic Drugs644

16.4.2 Structure-modifying Anti-inflammatory Drugs645

16.5 Conclusions and Future Directions648

16.6 Problems649

References649

本章重点内容651

索引653