Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization /

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasin...

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Bibliographic Details
Main Author: Kerns, Edward Harvel
Corporate Author: ScienceDirect (Online service)
Other Authors: Di, Li
Format: eBook
Language:English
Published: Amsterdam ; Boston : Academic Press, [2008]
Subjects:
Online Access:Connect to the full text of this electronic book
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MARC

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245 1 0 |a Drug-like properties :  |b concepts, structure design and methods : from ADME to toxicity optimization /  |c Edward H. Kerns and Li Di. 
264 1 |a Amsterdam ;  |a Boston :  |b Academic Press,  |c [2008] 
264 4 |c ©2008 
300 |a xix, 526 pages, 2 unnumbered pages of plates :  |b illustrations (some color) ;  |c 27 cm. 
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520 |a Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. * Serves as an essential working handbook aimed at scientists and students in medicinal chemistry * Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies * Discusses improvements in pharmacokinetics from a practical chemist's standpoint. 
505 0 |a Preface; Introductory Concepts; Physicochemical Properties; Disposition, Metabolism and Safety; Methods; Specific Topics; Answers to Problems; Appendix I: General References; Appendix II: Glossary. 
504 |a Includes bibliographical references (page 492) and index. 
500 |a Electronic resource. 
650 0 |a Pharmaceutical chemistry. 
650 0 |a Drugs  |x Structure-activity relationships. 
650 0 |a Drug development. 
650 0 |a Drugs  |x Design. 
650 1 2 |a Drug Design. 
650 2 2 |a Drug Evaluation, Preclinical. 
650 2 2 |a Drug-Related Side Effects and Adverse Reactions. 
650 2 2 |a Pharmaceutical Preparations  |x metabolism. 
650 2 2 |a Pharmacokinetics. 
650 2 2 |a Structure-Activity Relationship. 
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