For over half a century, this book has served the discipline of medicinal chemistry for both graduate and undergraduate pharmacy and chemistry students as well as practicing pharmacists. Fully updated for the Twelfth Edition, coverage begins with the fundamental principles of chemistry, biochemistry, and biology that underlie the discipline of medicinal chemistry. These principles are then applied to understanding the properties, mode of action, therapeutic applications, and limitations of various pharmaceutical agents. The subject matter is organized by pharmaceutical and therapeutic classes, providing a bridge between the basic sciences and clinical practice. The text contains many tables for quick reference to names, formulations, dosages, and applications. This edition includes chapter review questions.

A companion website provides answers to the review questions for students and an image bank for faculty.

1. Introduction
2. Drug Design Strategies
3. Metabolic Changes of Drugs and Related Organic Compounds
4. Biotechnology and Drug Discovery
5. Immunobiologicals
6. Anti-infective
7. Antimalarials
8. Antibacterial Antibiotics
9. Antiviral Agents
10. Antineoplastic Agents
11. Agents for Diagnostic Imaging
12. Central Nervous System Depressant
13. Central Dopaminergic Signaling Agents
14. Anticonvulsants
15. Central Nervous System Stimulants
16. Adrenergic Agents
17. Cholinergic Drugs
18. Renal Acting Agents
19. Cardiovascular Agents
20. Hormone Related Disorders: Nonsteroidal Therapies
21. Agents Treating Bone Disorders
22. Anesthetics
23. Histamine and Antihistaminic Agents
24. Analgesics
25. Steroids and Therapeutically Related Compounds
26. Prostaglandins, Leukotrienes, and Other Eicosanoids
27. Proteins, Enzymes and Peptide Hormones
28. Vitamins and Related Compounds
29. An Introduction to the Medicinal Chemistry of Herbs

Appendix, Calculated Log 0, Log D and pKa