Patrick- Medicinal Chemistry

Brief contents

List of boxes xix

Acronyms and abbreviations xxi

1 Drugs and drug targets: an overview 1

PART A Drug targets

2 Protein structure and function 17

3 Enzymes: structure and function 30

4 Receptors: structure and function 42

5 Receptors and signal transduction 58

6 Nucleic acids: structure and function 71

PART B Pharmacodynamics and pharmacokinetics

7 Enzymes as drug targets 87

8 Receptors as drug targets 102

9 Nucleic acids as drug targets 120

10 Miscellaneous drug targets 135

11 Pharmacokinetics and related topics 153

■ Case study 1: Statins 178

PART C Drug discovery, design, and development

12 Drug discovery: finding a lead 189

13 Drug design: optimizing target interactions 215

14 Drug design: optimizing access to the target 248

15 Getting the drug to market 274

■ Case study 2: The design of angiotensinconverting enzyme (ACE) inhibitors 292

■ Case study 3: Artemisinin and related antimalarial drugs 299

■ Case study 4: The design of oxamniquine 305

PART D Tools of the trade

16 Combinatorial and parallel synthesis 313

17 Computers in medicinal chemistry 337

18 Quantitative structure-activity relationships

(QSAR) 383

■ Case study 5: Design of a thymidylate synthase

inhibitor 407

PART E Selected topics in medicinal chemistry

19 Antibacterial agents 413

20 Antiviral agents 468

21 Anticancer agents 514

22 Cholinergics, anticholinergics, and

anticholinesterases 578

23 Drugs acting on the adrenergic

nervous system 609

24 The opioid analgesics 632

25 Anti-ulcer agents 659

■ Case study 6: Steroidal anti-inflammatory agents 689

■ Case Study 7: Current research into

antidepressant agents 700

Appendix 1 Essential amino acids 705

Appendix 2 The standard genetic code 706

Appendix 3 Statistical data for quantitative

structure-activity relationships (QSAR) 707 Appendix 4 Theactionof nerves 711

Appendix 5 Microorganisms 715

Appendix 6 Drugs and their trade names 717

Appendix 7 Trade names and drugs 722

Appendix 8 Hydrogen bonding interactions 728

Appendix 9 Drug properties 730

Glossary 741

General further reading 761

Index 763