drug like properties concepts structure design and methods from adme to toxicity optimization

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Drug Like Properties Concepts Structure Design And Methods

Author : Li Di
ISBN : 9780080557618
Genre : Science
File Size : 84. 66 MB
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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

Drug Like Properties

Author : Li Di
ISBN : 9780128013229
Genre : Science
File Size : 58. 3 MB
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Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property. Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization. Provides a comprehensive and valuable working handbook for scientists and students in medicinal chemistry Includes expanded coverage of pharmacokinetics fundamentals and effects Contains updates throughout, including the authors’ recent work in the importance of solubility in drug development; new and currently used property methods, with a reduction of seldom-used methods; and exploration of computational modeling methods

Drug Like Properties Concepts Structure Design And Methods

Author : Edward Kerns
ISBN : 9780080951621
Genre : Medical
File Size : 20. 39 MB
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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

Chemistry Of Opioids

Author : Hiroshi Nagase
ISBN : 9783642181061
Genre : Science
File Size : 49. 48 MB
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Recent Advances in the Synthesis of Morphine and Related Alkaloids; by N. Chida * Opioids in Preclinical and Clinical Trials; by H. Nagase and H. Fujii * Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions; by H. Schmidhammer and M. Spetea * 14-Amino-4,5-Epoxymorphinan Derivatives and Their Pharmacological Actions; by J. W. Lewis and S. M. Husbands * Nonpeptidic Delta (δ) Opioid Agonists and Antagonists of the Diarylmethylpiperazine Class: What Have We Learned?; by S. N. Calderon * Synthesis of Neoclerodane Diterpenes and Their Pharmacological Effects; by K. M. Lovell, K. M. Prevatt-Smith, A. Lozama and T. E. Prisinzano * Synthesis of Novel Basic Skeletons Derived from Naltrexone; by H. Nagase and H. Fujii * Twin and Triplet Drugs in Opioid Research; by H. Fujii * 3D-Pharmacophore Identification for κ-Opioid Agonists Using Ligand-Based Drug-Design Techniques; by N. Yamaotsu and S. Hirono

Adme Enabling Technologies In Drug Design And Development

Author : Donglu Zhang
ISBN : 9781118180761
Genre : Science
File Size : 21. 99 MB
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A comprehensive guide to cutting-edge tools in ADME research The last decade has seen tremendous progress in the developmentof analytical techniques such as mass spectrometry and molecularbiology tools, resulting in important advances in drug discovery,particularly in the area of absorption, distribution, metabolism,and excretion (ADME). ADME-Enabling Technologies in Drug Design and Developmentfocuses on the current state of the art in the field, presenting acomprehensive review of the latest tools for generating ADME datain drug discovery. It examines the broadest possible range ofavailable technologies, giving readers the information they need tochoose the right tool for a given application, a key requisite forobtaining favorable results in a timely fashion for regulatoryfilings. With over thirty contributed chapters by an internationalteam of experts, the book provides: A thorough examination of current tools, covering bothelectronic/mechanical technologies and biologically based ones Coverage of applications for each technology, including keyparameters, optimal conditions for intended results, protocols, andcase studies Detailed discussion of emerging tools and techniques, from stemcells and genetically modified animal models to imagingtechnologies Numerous figures and diagrams throughout the text Scientists and researchers in drug metabolism, pharmacology,medicinal chemistry, pharmaceutics, toxicology, and bioanalyticalscience will find ADME-Enabling Technologies in Drug Design andDevelopment an invaluable guide to the entire drug developmentprocess, from discovery to regulatory issues.

Books In Print 2009 2010

Author :
ISBN : 0835250199
Genre : Publishers' catalogs
File Size : 54. 93 MB
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Mini Reviews In Medicinal Chemistry

Author :
ISBN : UCSC:32106017986636
Genre : Pharmaceutical chemistry
File Size : 71. 26 MB
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Wiley Encyclopedia Of Chemical Biology

Author : Tadhg P. Begley
ISBN : 0471754773
Genre : Science
File Size : 68. 53 MB
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Comprehensive Medicinal Chemistry Ii

Author : John B. Taylor
ISBN : 0080445136
Genre : Computers
File Size : 81. 20 MB
Format : PDF
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The first edition of Comprehensive Medicinal Chemistry was published in 1990 and very well received. Comprehensive Medicinal Chemistry II is much more than a simple updating of the contents of the first edition. Completely revised and expanded, this new edition has been refocused to reflect the significant developments and changes over the past decade in genomics, proteomics, bioinformatics, combinatorial chemistry, high-throughput screening and pharmacology, and more. The content comprises the most up-to-date, authoritative and comprehensive reference text on contemporary medicinal chemistry and drug research, covering major therapeutic classes and targets, research strategy and organisation, high-throughput technologies, computer-assisted design, ADME and selected case histories. It is this coverage of the strategy, technologies, principles and applications of medicinal chemistry in a single work that will make Comprehensive Medicinal Chemistry II a unique work of reference and a single point of entry to the literature for pharmaceutical and biotechnology scientists of all disciplines and for many industry executives as well.Comprehensive Medicinal Chemistry II will be available online in 2007 via the proven platform ScienceDirect providing the user with enhanced features such as cross-referencing and dynamic linking. * Comprehensively reviews - for the first time in one single work - the strategies, technologies, principles and applications of modern medicinal chemistry * Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets * Includes a unique collection of case studies and personal assays reviewing the discovery and development of key drugs

Comprehensive Medicinal Chemistry Ii Global Perspective

Author : John Bodenhan Taylor
ISBN : 0080445144
Genre : Medical
File Size : 61. 49 MB
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This e-book comprises 8 volumes, with all chapter sections available as PDF or HTML, and includes bibliographical references and index.

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