Provides drug discovery scientists and students with a practical understanding of property fundamentals, effects, structure-property relationships, and structure modification strategies that can be applied to improving drug leads.
Reviewer:Thomas L. Pazdernik, PhD(University of Kansas Medical Center)
Description:Two pharmaceutical scientists have put together this valuable summary of what needs to be known about drug chemical and physical properties and biological activities to optimize the process of drug discovery.
Purpose:The objective is to summarize information on ADME (absorption/distribution/metabolism/excretion) and toxic property concepts, structure design, and methodologies required to optimize the process of drug discovery. The authors have done a nice job of presenting this information in a concise and readable format.
Audience:This book will be of great value for both chemists and biologists who are in training for and/or are part of a drug discovery team.
Features:Each chapter starts with a bulleted outline of what is to be covered and ends with a problem set (answers in appendix I) to facilitate understanding of the material. Key references are provided at the end of each chapter. Part 1 of the book deals with introductory information on concepts that are used in drug discovery. Part 2 deals with the physicochemical property concepts of chemicals that must be understood to optimally develop a chemical entity into a useful drug. Part 3 deals with the important concepts that must be understood about drug distribution, metabolism, and safety. The concepts of pharmacokinetics are presented with a minimal of mathematics, focusing on their practical applications to drug discovery projects. Part 4 is devoted to key methods that are used in drug discovery. The book concludes with a special topics section including diagnosing and improving pharmacokinetic performance, prodrugs, effects of properties on biological assays and drug formulations. Appendix II contains a list of very general references and Appendix III is a glossary that defines important terms used in drug discovery.
Assessment:This is a valuable reference for any scientist who works as part of a drug discovery team and especially those who are involved in ADME to toxicity optimization.