Bibliothèque de L'IMIST/CNRST

Includes bibliographical references (page 492) and index.

Introductory Concepts -- 1. 2. Advantages of Good Drug-like Properties -- 3. Barriers to Drug Exposure in Living Systems -- Physicochemical Properties -- 4. Rules for Rapid Property Profiling from Structure -- 5. Lipophilicity -- 6. pK[subscript a] -- 7. Solubility -- 8. Permeability -- Disposition, Metabolism, and Safety -- 9. Transporters -- 10. Blood-Brain Barrier -- 11. Metabolic Stability -- 12. Plasma Stability -- 13. Solution Stability -- 14. Plasma Protein Binding -- 15. Cytochrome P450 Inhibition -- 16. hERG Blocking -- 17. Toxicity -- 18. Integrity and Purity -- 19. Pharmacokinetics -- 20. Lead-like Compounds -- 21. Strategies for Integrating Drug-like Properties into Drug Discovery -- Methods -- 22. Methods for Profiling Drug-like Properties: General Concepts -- 23. Lipophilicity Methods -- 24. pK[subscript a] Methods -- 25. Solubility Methods -- 26. Permeability Methods -- 27. Transporter Methods -- 28. Blood-Brain Barrier Methods -- 29. Metabolic Stability Methods -- 30. Plasma Stability Methods -- 32. CYP Inhibition Methods -- 33. Plasma Protein Binding Methods -- 34. hERG Methods -- 35. Toxicity Methods -- 36. Integrity and Purity Methods -- 37. Pharmacokinetic Methods -- Specific Topics -- 38. Diagnosing and Improving Pharmacokinetic Performance -- 39. Prodrugs -- 40. Effects of Properties on Biological Assays -- 41. Formulation -- App. I. Answers to Chapter Problems -- App. II. General References -- App. III. Glossary.

"This book explains the drug discovery process and how property-based design can increase the success rate of bringing compounds to market. Written from the perspective of a drug discovery scientist, it is a practical guide for medicinal and pharmaceutical chemists, ADME scientists (who study the absorption, distribution, metabolism, and excretion of pharmaceuticals) and advanced students in these fields."--Jacket.