Combinatorial Chemistry And Molecular Diversity In Drug Discovery
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Combinatorial Chemistry And Molecular Diversity In Drug Discovery
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Author : Eric M. Gordon
language : en
Publisher: Wiley-Liss
Release Date : 1998-08-27
Combinatorial Chemistry And Molecular Diversity In Drug Discovery written by Eric M. Gordon and has been published by Wiley-Liss this book supported file pdf, txt, epub, kindle and other format this book has been release on 1998-08-27 with Medical categories.
Increasing pressure to identify, optimize, develop, and commercialize novel drugs more rapidly and more cost-effectively has led to an urgent demand for technologies that can reduce the time to market for new products. Molecular diversity, of both natural and synthetic materials, provides a valuable source of compounds for identifying and optimizing new drug leads. Through the rapidly evolving technology of combinatorial chemistry, it is now possible to produce libraries of small molecules to screen for novel bioactivities. This powerful new technology has begun to help pharmaceutical companies find new drug candidates quickly, save significant dollars in preclinical development costs, and ultimately change their fundamental approach to drug discovery. Included among the many topics: Historical background. Library strategy and design. Solid-phase synthesis. Small molecular libraries. Automation, analytical, and computational methodology. Biological diversity. Strategies for screening combinatorial libraries. Combinatorial drug screening and development. Combinatorial chemistry information management.
Molecular Diversity In Drug Design
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Author : P.M. Dean
language : en
Publisher: Springer Science & Business Media
Release Date : 1999-10-31
Molecular Diversity In Drug Design written by P.M. Dean and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 1999-10-31 with Medical categories.
This book focuses on the theoretical problems associated with molecular diversity as it is being applied in the pharmaceutical industry. Therefore, this book deals with algorithms that are involved in understanding chemical space and selection of diverse sets of structures. The algorithms also deal with the problem of focused diversity where chemical libraries are being created within a structured physical volume. Diversity is necessarily connected to combinational chemistry, although this book is limited to the application of diversity methods to combinational chemistry and does not deal with synthetic methods. It is this focus on algorithms and strategies for exploiting molecular diversity that makes it different from books on combinational chemistry. The intended readership of the book falls into two categories: those actively engaged in applying molecular diversity in the chemical industry and those in academia who are developing strategies to embrace, understand and accept the many problems thrown up by this new research field of molecular diversity.
Molecular Diversity In Drug Design
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Author : P.M. Dean
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-05-08
Molecular Diversity In Drug Design written by P.M. Dean and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-05-08 with Science categories.
High-throughput screening and combinatorial chemistry are two of the most potent weapons ever to have been used in the discovery of new drugs. At a stroke, it seems to be possible to synthesise more molecules in a month than have previously been made in the whole of the distinguished history of organic chemistry, Furthermore, all the molecules can be screened in the same short period. However, like any weapons of immense power, these techniques must be used with care, to achieve maximum impact. The costs of implementing and running high-throughput screening and combinatorial chemistry are high, as large dedicated facilities must be built and staffed. In addition, the sheer number of chemical leads generated may overwhelm the lead optimisation teams in a hail of friendly fire. Mother nature has not entirely surrendered, as the number of building blocks that could be used to build libraries would require more atoms than there are in the universe. In addition, the progress made by the Human Genome Project has uncovered many proteins with different functions but related binding sites, creating issues of selectivity. Advances in the new field of pharmacogenomics will produce more of these challenges. There is a real need to make hi- throughput screening and combinatorial chemistry into 'smart' weapons, so that their power is not dissipated. That is the challenge for modellers, computational chemists, cheminformaticians and IT experts. In this book, we have broken down this grand challenge into key tasks.
Diversity Oriented Synthesis
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Author : Andrea Trabocchi
language : en
Publisher: John Wiley & Sons
Release Date : 2013-06-17
Diversity Oriented Synthesis written by Andrea Trabocchi and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-06-17 with Science categories.
Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.
Combinatorial Library
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Author : Lisa B. English
language : en
Publisher: Springer Science & Business Media
Release Date : 2008-02-04
Combinatorial Library written by Lisa B. English and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-02-04 with Science categories.
The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.
Annual Reports In Combinatorial Chemistry And Molecular Diversity
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Author : M.R. Pavia
language : en
Publisher: Springer
Release Date : 1999-06-30
Annual Reports In Combinatorial Chemistry And Molecular Diversity written by M.R. Pavia and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 1999-06-30 with Science categories.
Combinatorial chemistry and molecular diversity approaches to scientific and novel product R & D have exploded in the 1990s. For example, in the preparation of drug candidates, the automated, permutational, and combinatorial use of chemical building blocks now allows the generation and screening of unprecedented numbers of compounds. Drug discovery - better, faster, cheaper? Indeed more compounds have been made and screened in the 1990s than in the last hundred years of pharmaceutical research. The second volume in this series includes contributions on methods, solid phases, purification, analysis, carbohydrates, patent strategies and tactics, diversity profiling and combinatorial series design, and finishes with a survey of chemical libraries yielding biologically active agents and a compendium of solid phase chemistry publications. Each contribution is prepared by a recognized expert resulting in a high quality account of the recent advances in the field.
Molecular Diversity And Combinatorial Chemistry
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Author : Irwin M. Chaiken
language : en
Publisher:
Release Date : 1996
Molecular Diversity And Combinatorial Chemistry written by Irwin M. Chaiken and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 1996 with Medical categories.
Reports progress on chemical, enzymatic, phage, and cell-derived libra ries. Discusses synergy between structure-based design and combinatori al libraries. Presents applications of combinatorial libraries to drug discovery and new synthetic catalysis. Reports library screening appr oaches, including the use of NMR. Presents recent advances in solid-ph ase organic synthesis, liquid-phase organic synthesis, and high-throug hput combinatorial organic synthesis. Discusses automation of organic synthesis as well as new methodologies for monitoring solid-phase orga nic synthesis.
Annual Reports In Combinatorial Chemistry And Molecular Diversity
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Author : M.R. Pavia
language : en
Publisher: Springer Science & Business Media
Release Date : 2013-04-18
Annual Reports In Combinatorial Chemistry And Molecular Diversity written by M.R. Pavia and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-04-18 with Science categories.
Combinatorial chemistry and molecular diversity approaches to scientific and novel product R & D have exploded in the 1990s. For example, in the preparation of drug candidates, the automated, permutational, and combinatorial use of chemical building blocks now allows the generation and screening of unprecedented numbers of compounds. Drug discovery - better, faster, cheaper? Indeed more compounds have been made and screened in the 1990s than in the last hundred years of pharmaceutical research. The second volume in this series includes contributions on methods, solid phases, purification, analysis, carbohydrates, patent strategies and tactics, diversity profiling and combinatorial series design, and finishes with a survey of chemical libraries yielding biologically active agents and a compendium of solid phase chemistry publications. Each contribution is prepared by a recognized expert resulting in a high quality account of the recent advances in the field.
Drug Discovery And Development Volume 1
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Author : Mukund S. Chorghade
language : en
Publisher: John Wiley & Sons
Release Date : 2006-07-18
Drug Discovery And Development Volume 1 written by Mukund S. Chorghade and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-07-18 with Science categories.
From first principles to real-world applications -- here is the first comprehensive guide to drug discovery and development Modern drug discovery and development require the collaborative efforts of specialists in a broadarray of scientific, technical, and business disciplines--from biochemistry to molecular biology, organic chemistry to medicinal chemistry, pharmacology to marketing. Yet surprisingly, until now, there were no authoritative references offering a complete, fully integrated picture of the process. The only comprehensive guide of its kind, this groundbreaking two-volume resource provides an overview of the entire sequence of operations involved in drug discovery and development--from initial conceptualization to commercialization to clinicians and medical practitioners. Volume 1: Drug Discovery describes all the steps in the discovery process, including conceptualizing a drug, creating a library of candidates for testing, screening candidates for in vitro and in vivo activity, conducting and analyzing the results of clinical trials, and modifying a drug as necessary. Volume 2: Drug Development delves into the nitty-gritty details of optimizing the synthetic route, drug manufacturing, outsourcing, and marketing--including drug coloring and delivery methods. Featuring contributions from a world-class team of experts, Drug Discovery and Development: * Features fascinating case studies, including the discovery and development of erythromycin analogs, Tagamet, and Ultiva (remifentanil) * Discusses the discovery of medications for bacterial infections, Parkinson's disease, psoriasis, peptic ulcers, atopic dermatitis, asthma, and cancer * Includes chapters on combinatorial chemistry, molecular biology-based drug discovery, genomics, and chemogenomics Drug Discovery and Development is an indispensable working resource for industrialchemists, biologists, biochemists, and executives who work in the pharmaceutical industry.
Integrated Drug Discovery Technologies
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Author : Houng-Yau Mei
language : en
Publisher: CRC Press
Release Date : 2002-03-19
Integrated Drug Discovery Technologies written by Houng-Yau Mei and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2002-03-19 with Science categories.
Integrated Drug Discovery Technologies provides a global overview of emerging drug development technologies by presenting and integrating new techniques from the disciplines of chemistry, biology, and computational sciences. It combines integration of contemporary mechanization with strategies in drug delivery. Topics include: functional genomics, microfabrication techniqes, integrated proteomics technologies, high throughput screening, and fluorescence correlation spectroscopy methods.