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药物化学 英汉双语教材 英中双语注解版pdf电子书版本下载
- 李绍顺编著 著
- 出版社： 北京：科学出版社
- ISBN：9787030247872
- 出版时间：2009
- 标注页数：662页
- 文件大小：37MB
- 文件页数：694页
- 主题词：药物化学－英、汉
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图书目录
Chapter 1 Drug Discovery,Design and Development 1
1.1 Drug Discovery 1
1.1.1 ADrug Discovery Without a Lead 2
1.1.2 Lead Discovery 5
1.2 Lead Modification 9
1.2.1 Identification of the Active Part:The Pharmacophore 9
1.2.2 Structure Modifications to Increase Potency and the Therapeutic Index 12
1.3 Structure-Activity Relationships 21
1.4 Quantitative Structure-Activity Relationships 23
1.4.1 Methods Used to Correlate Physicochemical Parameters with Biological Activity:2D-QSAR 24
1.4.2 Computer-Based Methods of QSAR Related to Receptor Binding:3D-QSAR 26
1.4.3 Structure-Based Drug Design 29
1.5 New Drug Development 36
1.5.1 General Process of New Drug Development 36
1.5.2 Preclinical Development and Investigational New Drug Application 38
1.6 Problems 39
本章重点内容 40
Chapter 2 Receptors 42
2.1 Drug-Receptor Interactions 42
2.1.1 Interactions(Forces)Involved in the Drug-Receptor Complex 42
2.2 Theories for Drug-Receptor Interactions 51
2.2.1 Occupancy Theory 51
2.2.2 Rate Theory 53
2.2.3 Induced-Fit Theory 53
2.2.4 Macromolecular Perturbation Theory 54
2.2.5 Activation-Aggregation Theory 55
2.2.6 The Two-State(Multistate)Model of Receptor Activation 55
2.3 Topographical and Stereochemical Considerations 57
2.3.1 Spatial Arrangement of Atoms 57
2.3.2 Drug and Receptor Chirality 58
2.3.3 Geometric Isomers(Diastereomers) 69
2.3.4 Conformational Isomers 70
2.3.5 Ring Topology 76
2.4 Problems 77
本章重点内容 80
Chapter 3 Enzymes and Enzyme Inhibition 83
3.1 Enzymes 83
3.1.1 Enzymes as Catalysts 83
3.1.2 Mechanisms of Enzyme Catalysis 88
3.1.3 Coenzyme Catalysis 92
3.2 Enzyme Inhibition 95
3.2.1 Enzyme Inhibitors in Medicine 95
3.2 2 Design of Enzyme Inhibitors 96
3.3 Reversible Enzyme Inhibitors 99
3.3.1 Mechanism of Reversible Inhibition 99
3.3.2 Selected Examples of Competitive Reversible Inhibitor Drugs 101
3.3.3 Transition State Analogs 103
3.3.4 Multisubstrate Analogs 105
3.3.5 Slow,Tight-Binding Inhibitors 106
3.4 Irreversible Enzyme Inhibitors 108
3.4.1 Affinity Labeling Agents 108
3.4.2 Mechanism-Based Enzyme Inactivators 111
3.5 Problems 114
本章重点内容 116
Chapter 4 Drug Metabolism 118
4.1 Introduction 118
4.1.1 Definition of Drug Metabolism 118
4.1.2 Site of Drug Metabolism and First-Pass Effect 118
4.1.3 Purpose of Drug Metabolism Studies 119
4.1.4 Function of Drug Metabolism and Categories of Drug Metabolism Reaction 120
4.2 Phase Ⅰ Transformations 121
4.2.1 Oxidative Reactions 121
4.2.2 Reductive Reactions 135
4.2.3 Carboxylation Reaction 139
4.2.4 Hydrolytic Reactions 140
4.3 Phase Ⅱ Transformations:Conjugation Reactions 141
4.3.1 Introduction 141
4.3.2 Glucuronic Acid Conjugation 143
4.3.3 Sulfate Conjugation 145
4.3.4 Amino Acid Conjugation 146
4.3.5 Glutathione Conjugation 148
4.3.6 Acetyl Conjugation 150
4.3.7 Other Conjugation 152
4.4 Problems 153
本章重点内容 155
Chapter 5 Prodrugs and Drug Delivery Systems 157
5.1 Enzyme Activation of Drugs 157
5.1.1 Utility of Prodrugs 157
5.1.2 Types of Prodrugs 159
5.2 Mechanisms of Drug Activation 160
5.2.1 Carrier-Linked Prodrugs 160
5.2.2 Bioprecursor Prodrugs 177
5.3 Problems 189
本章重点内容 190
Chapter 6 Central Nervous System Drugs 191
6.1 Schizophrenia 191
6.1.1 Introduction 191
6.1.2 Disease Basis 191
6.1.3 Current Treatment 193
6.1.4 Stucture-activity Relationship of Tricyclic Anti-psychotics 197
6.1.5 Unmet Medical Needs 201
6.1.6 New Research Areas 202
6.2 Affective Disorders:Depression and Bipolar Disease 203
6.2.1 Introduction 203
6.2 2 Disease Basis 204
6.2.3 Current Treatment 204
6.2.4 Stucture-activity Relationship of Tricyclic antidepressants 209
6.2.5 Unmet Medical Needs 211
6.2.6 New Research Areas 211
6.3 Anxiety 212
6.3.1 Introduction 212
6.3.2 Disease Basis 213
6.3.3 Current Treatments 213
6.3.4 Stucture-activity Relationship of Benzodiazepines 216
6.3.5 New Research Areas 218
6.4 Sleep Disorders 218
6.4.1 Introduction 218
6.4.2 Disease Basis 219
6.4.3 Current Treatment 219
6.4.4 Unmet Medical Needs 225
6.4.5 New Research Areas 225
6.5 Epilepsy 225
6.5.1 Introduction 225
6.5.2 Disease Basis 226
6.5.3 Current Treatment 226
6.5.4 Stucture-activity Relationship on homotypical drugs of Barbiturates 228
6.5.5 Unmet Medical Needs 229
6.5.6 New Research Areas 230
6.6 Addiction 231
6.6.1 Introduction 231
6.6.2 Disease Basis 233
6.6.3 Current Treatment 234
6.6.4 Unmet Medical Needs 236
6.6.5 New Research Areas 236
6.7 Neurodegeneration 236
6.7.1 Overview 236
6.7.2 Alzheimer's Disease 238
6.7.3 Parkinson's Disease 248
6.7.4 Future Aspects 253
6.8 Problems 254
References 254
本章重点内容 255
Chapter 7 Analgesics and Anesthetics 258
7.1 Analgesics 258
7.1.1 Introduction 258
7.1.2 Opioid Receptor 260
7.1.3 Endogenous Opioid Peptides 260
7.1.4 Morphine and Related Opioids 261
7.1.5 Synthesis Analgesics 265
7.1.6 Opioid Agonist/Antagonists and Partial Agonists 270
7.1.7 Opioid Antagonists 270
7.1.8 Structure-Activity Relationships 271
7.1.9 Unmet Medical Needs 273
7.1.10 New Research Areas 273
7.2 Anesthetics 274
7.2.1 General Anesthetics 274
7.2.2 Local Anesthetics 279
7.2.3 Unmet Medical Needs 287
7.2.4 New Research Areas 288
7.3 Problem 289
本章重点内容 290
Chapter 8 Drugs for Metabolic Syndrome Treatment 292
8.1 Introduction 292
8.1.1 Definition of Metabolic Syndrome(Mats) 292
8.1.2 Management of the Metabolic Syndrome 292
8.2 Obesity/Disorders of Energy 293
8.2.1 Disease State 293
8.2.2 Disease Basis 294
8.2.3 Current Treatment 294
8.2.4 Unmet Medical Needs 299
8.2.5 New Research Areas 302
8.3 Diabetes 308
8.3.1 Introduction 308
8.3.2 Disease Basis 309
8.3.3 Current Treatment 313
8.3.4 Unmet Medical Needs 327
8.3.5 New Research Areas 328
8.4 Problems 332
References 332
本章重点内容 333
Chapter 9 Agents for Gastrointestinal Diseases 335
9.1 Introduction 335
9.1.1 The Function of Gastrointestinal Tract 335
9.1.2 Historical Overview 335
9.2 Gastric and Mucosal Ulceration 338
9.2.1 Overview 338
9.2.2 Disease Basis 338
9.2.3 Current Treatment 339
9.2.4 Unmet Medical Needs 348
9.2.5 New Research Areas 349
9.3 Inflammatory Bowel Disease 349
9.3.1 Overview 349
9.3.2 Disease Basis 350
9.3.3 Current Treatment 351
9.3.4 Unmet Medical Needs 355
9.3.5 New research Areas 355
9.4 Emesis/Prokinetic Agents 358
9.4.1 Overview 358
9.4.2 Disease Basis 358
9.4.3 Current Treatment 360
9.4.4 Unmet Medical Needs 368
9.4.5 New research Areas 368
9.5 Problems 369
References 369
本章重点内容 370
Chapter 10 Cardiovascular Agents 372
10.1 Introduction 372
10.2 Hypertension 372
10.2.1 Disease Basis 372
10.2.2 Current Antihypertensive Agents 374
10.2.3 Unmet Medical Needs 396
10.2.4 New Research Areas 397
10.3 Cardiac Arrhythmias 397
10.3.1 Disease Basis 397
10.3.2 Current Anti-arrhythmic Agents 398
10.3.3 Unmet Medical Needs 406
10.3.4 New Research Areas 406
10.4 Congestive Heart Failure 407
10.4.1 Disease Basis 407
10.4.2 Current Cardiac Agents 407
10.5 Angina 411
10.5.1 Disease Basis 411
10.5.2 Current Anti-anginal Agents 411
10.6 Hyperlipidemias 413
10.6.1 Disease Basis 413
10.6.2 Anti-hyperlipidemic Agents 415
10.7 Problems 424
References 424
选读资料 425
本章重点内容 426
Chapter 11 Anticancer Agents 429
11.1 Introduction 429
11.2 Alkylating and Platinum Anticancer Agents 429
11.2.1 Current Treatments 430
11.2.2 Platinum Complexes 439
11.3 Deoxyribonucleic Acid Topoisomerase Inhibitors 441
11.3.1 Topoisomerase Ⅰ Inhibitors Camptothecin and Analogs 442
11.3.2 Topoisomerase Ⅱ Inhibitors 443
11.4 Antimetabolites 449
11.4.1 Current Treatment 449
11.5 Microtubule Targeting Agents 457
11.5.1 Inhibitors of Microtubule Assembly 458
11.5.2 Microtubule Stabilizers 460
11.6 Unmet Medical Needs and New Research Areas 462
11.6.1 Tyrosine Kinase and Inhibitors 463
11.6.2 Multi-targeted Kinase Inhibitors 465
11.6.3 Histone Deacetylase Inhibitors 466
11.6.4 Proteasome Inhibitors 467
11.6.5 Other New Research Areas 468
11.7 Problems 469
References 469
本章重点内容 470
Chapter 12 Antiviral 472
12.1 Antivirals for Herpesviruses 472
12.1.1 Introduction 472
12.1.2 Disease Basis 473
12.1.3 Current Treatment 473
12.1.4 Structure-activity Relationship 477
12.1.5 Unmet Medical Needs 480
12.1.6 New Research Areas 480
12.2 Antivirals for Human Immunodeficiency Virus 481
12.2.1 Introduction 481
12.2.2 Disease Basis 481
12.2.3 Current Treatment 482
12.2.4 Structure-activity Relationship 488
12.2.5 Unmet Medical Needs 492
12.2.6 New Research Areas 493
12.3 Antivirals for Influenza Virus 496
12.3.1 Introduction 496
12.3.2 Disease Basis 496
12.3.3 Current Treatment 497
12.3.4 Structure-activity Relationship 500
12.3.5 Unmet Medical Needs 504
12.3.6 New Research Areas 504
12.4 Problems 505
选读资料 505
本章重点内容 506
Chapter 13 Antifungal Agents 508
13.1 Introduction 508
13.1.1 General Classification and Structure of Medically Important Fungi 508
13.1.2 Human Pathogenic Fungi and Disease States 509
13.2 Current Antifungal Agents 511
13.2.1 General 511
13.2.2 The Mechanism of Action 512
13.3 Typical Antifungal Drugs in Clinical Use 513
13.3.1 Amphotericin B 513
13.3.2 Azoles 516
13.3.3 Allylamines 522
13.4 New Research Areas 525
13.4.1 Overview 525
13.4.2 Isoleucyl-tRNA Synthetase Inhibitors(ITRS) 525
13.4.3 Sphingolipid Biosynthesis Inhibitors 526
13.5 Problems 527
本章重点内容 528
Chapter 14 Antibacterials 529
14.1 Introduction 529
14.2 β-lactam 532
14.2.1 History and Overview 532
14.2.2 Mode of Action 534
14.2.3 Mechanisms of Resistance 537
14.2.4 Major Drug Classes 539
14.3 Macrolide 547
14.3.1 Introduction 547
14.3.2 Mechanism of Action 548
14.3.3 Major Classes of Macrolides 551
14.4 Tetracyclines 557
14.4.1 Introduction 557
14.4.2 SAR of Tetracyclines 558
14.4.3 Mechanism of Action 559
14.4.4 Major Classes of Tetracyclines 561
14.4.5 Antibacterial Resistance to the Tetracyclines 563
14.5 Quinolones 565
14.5.1 Overview of Quinolones 565
14.5.2 Mechanism of Antibacterial Action 567
14.5.3 SAR and STR of Quinolones 568
14.5.4 Antibacterial Resistance Mechanisms 568
14.5.5 Synthesis of Quinolones 568
14.6 Oxazolidinone 571
14.6.1 Introduction 571
14.6.2 SAR Leading to DuP-721 and DuP-105 572
14.6.3 SAR Leading to Eperezolid and Linezolid 572
14.6.4 Synthesis of Linezolid 574
14.6.5 Mode of Action 575
14.7 Aminoglycosides,glycopeptides,and others 575
14.7.1 Vancomycin 575
14.7.2 Aminoglycosides 576
14.7.3 Dapotamycin 578
14.8 Antimycobacterium Agents 579
14.8.1 Introduction 579
14.8.2 Rifamycin 581
14.8.3 Isoniazid 581
14.9 Resistance and Challenge[3] 583
14.10 Problems 585
References 585
本章重点内容 586
Chapter 15 Antiparasitics 589
15.1 Introduction 589
15.2 Representative Diseases 590
15.2.1 African Trypanosomiasis 590
15.2.2 Chagas disease 591
15.2.3 Leishmaniasis 592
15.2.4 Malaria 593
15.3 Antimalarias 594
15.3.1 Quinolines 596
15.3.2 Artemisinin and its analogs 600
15.4 Problems 604
References 605
本章重点内容 606
Chapter 16 Inflammatory Diseases and Nonsteroidal Anti-inflammatory Drugs(NSAIDs) 608
16.1 Introduction 608
16.1.1 Arthritis 609
16.1.2 Other Inflammatory and Immunological Diseases 612
16.2 Disease Basis 614
16.2.1 Arachidonic Acid Cascade 614
16.2.2 Phospholipase A2(PLA2) 616
16.2.3 Cyclooxygenase(COX) 618
16.2.4 Lipoxygenase(LOX) 619
16.3 Current Treatment for Arthritis 620
16.3.1 Steroids(Brief Introduction) 620
16.3.2 Nonsteroidal Anti-inflammatory Drugs(NSAIDs) 622
16.4 New Research Areas 644
16.4.1 Disease-modifying Anti-rheumatic Drugs 644
16.4.2 Structure-modifying Anti-inflammatory Drugs 645
16.5 Conclusions and Future Directions 648
16.6 Problems 649
References 649
本章重点内容 651
索引 653