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Combinatorial Synthesis Of Natural Product Based Libraries
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Book Synopsis Combinatorial Synthesis of Natural Product-Based Libraries by : Armen M. Boldi
Download or read book Combinatorial Synthesis of Natural Product-Based Libraries written by Armen M. Boldi and published by CRC Press. This book was released on 2006-05-16 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinato
Book Synopsis Combinatorial Library by : Lisa B. English
Download or read book Combinatorial Library written by Lisa B. English and published by Springer Science & Business Media. This book was released on 2008-02-04 with total page 380 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Combinatorial Synthesis of Natural Product-Based Libraries by : Armen M. Boldi
Download or read book Combinatorial Synthesis of Natural Product-Based Libraries written by Armen M. Boldi and published by CRC Press. This book was released on 2006-05-16 with total page 363 pages. Available in PDF, EPUB and Kindle. Book excerpt: Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinato
Book Synopsis Classics in Total Synthesis by : K. C. Nicolaou
Download or read book Classics in Total Synthesis written by K. C. Nicolaou and published by John Wiley & Sons. This book was released on 1996-04-11 with total page 826 pages. Available in PDF, EPUB and Kindle. Book excerpt: K.C. Nicolaou - Winner of the Nemitsas Prize 2014 in Chemistry This book is a must for every synthetic chemist. With didactic skill and clarity, K. C. Nicolaou and E. Sorensen present the most remarkable and ingenious total syntheses from outstanding synthetic organic chemists. To make the complex strategies more accessible, especially to the novice, each total synthesis is analyzed retrosynthetically. The authors then carefully explain each synthetic step and give hints on alternative methods and potential pitfalls. Numerous references to useful reviews and the original literature make this book an indispensable source of further information. Special emphasis is placed on the skillful use of graphics and schemes: Retrosynthetic analyses, reaction sequences, and stereochemically crucial steps are presented in boxed sections within the text. For easy reference, key intermediates are also shown in the margins. Graduate students and researchers alike will find this book a gold mine of useful information essential for their daily work. Every synthetic organic chemist will want to have a copy on his or her desk.
Book Synopsis Combinatorial Chemistry and Technologies by : Stanislav Miertus
Download or read book Combinatorial Chemistry and Technologies written by Stanislav Miertus and published by CRC Press. This book was released on 2005-04-12 with total page 597 pages. Available in PDF, EPUB and Kindle. Book excerpt: Several books on the market cover combinatorial techniques, but they offer just a limited perspective of the field, focusing on selected aspects without examining all approaches and integrated technologies. Combinatorial Chemistry and Technologies: Methods and Applications answers the demand for a complete overview of the field, covering all of the
Book Synopsis Combinatorial Chemistry by : Stephen R. Wilson
Download or read book Combinatorial Chemistry written by Stephen R. Wilson and published by John Wiley & Sons. This book was released on 1997-03-28 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: The new time-saving revolution in drug discovery. Combinatorial chemistry, a method for synthesizing millions of chemical compounds much faster than usual, is becoming one of the most useful technical tools available to chemists and researchers working today. Using current advances in computer and laboratory techniques, combinatorial chemistry has freed professionals from the drudgery of piecemeal experimental work and opened new creative possibilities for experimentation. Combinatorial Chemistry: Synthesis and Application details critical aspects of the technique, featuring the work of some of the world's leading chemists, many of whom played a key role in its development. Including examples of both solution-phase and solid-phase approaches as well as the full complement of organic chemistry technologies currently available, the book describes: * Concepts and terms of combinatorial chemistry * Polymer-supported synthesis of organic compounds * Macro beads as microreactors * Solid-phase methods in combinatorial chemistry * Encoded combinatorial libraries, including Rf-encoding of synthesis beads * Strategies for combinatorial libraries of oligosaccharides * Combinatorial libraries of peptides, proteins, and antibodies using biological systems. While combinatorial chemistry originated in peptide chemistry, this volume has deliberately focused on nonpeptide organic applications, illustrating the technique's wide uses. Combinatorial Chemistry introduces organic, medicinal, and pharmaceutical chemists as well as biochemists to this exciting, cost-effective, and practical technique, which has unlocked creative potential for the next millennium.
Book Synopsis Chemogenomics in Drug Discovery by : Hugo Kubinyi
Download or read book Chemogenomics in Drug Discovery written by Hugo Kubinyi and published by John Wiley & Sons. This book was released on 2006-03-06 with total page 487 pages. Available in PDF, EPUB and Kindle. Book excerpt: Chemogenomics brings together the most powerful concepts in modern chemistry and biology, linking combinatorial chemistry with genomics and proteomics. This first reference devoted to the topic covers all stages of the early drug discovery process, from target selection to compound library and lead design. With the combined expertise of 20 research groups from academia and leading pharmaceutical companies, this is a must-have for every drug developer and medicinal chemist applying the powerful methods of chemogenomics to speed up the drug discovery process.
Book Synopsis Molecular Diversity and Combinatorial Chemistry by : Irwin M. Chaiken
Download or read book Molecular Diversity and Combinatorial Chemistry written by Irwin M. Chaiken and published by . This book was released on 1996 with total page 346 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Combinatorial Chemistry and Molecular Diversity in Drug Discovery by : Eric M. Gordon
Download or read book Combinatorial Chemistry and Molecular Diversity in Drug Discovery written by Eric M. Gordon and published by Wiley-Liss. This book was released on 1998-08-27 with total page 552 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Synthesis and Structure Activity Relationship Studies of a Natural Product-derived Compound Library by : Paul Whitney Swain
Download or read book Synthesis and Structure Activity Relationship Studies of a Natural Product-derived Compound Library written by Paul Whitney Swain and published by . This book was released on 2010 with total page 351 pages. Available in PDF, EPUB and Kindle. Book excerpt: Infectious diseases will always be a public health concern. The incidence of bacterial strains found in clinical settings that exhibit resistance to our current arsenal of antimicrobial drugs has risen sharply in the past twenty years and is projected to keep rising. The Infectious Diseases Society of America (IDSA) stated that more people die of methicillin-resistant Staphylococcus aureus (MRSA) infections per year in US hospitals than HIV/AIDS and tuberculosis combined. However, stagnation of research in the area of infectious diseases over the past forty years has left us dreadfully behind in the battle against these deadly pathogens. Recently, researchers have started getting back to the roots of drug discovery by screening possible antibiotic-producing organisms isolated from the environment. Unfortunately this will take time as many of the more common antibiotics have already been found in this manner, leaving the rarest compounds to still be found. Other drug discovery programs focus on the production of large chemical libraries by combinatorial synthesis. While hundreds of thousands of compounds have been made in this way, only one FDA approved drug has been made by de novo synthesis. Compounds made by combinatorial methods lack much of the complexity afforded by natural products. Yet, it is the complexity of natural products that makes them good antibiotics. The strategy we employ is to use natural products in the synthesis of combinatorial libraries. In this manner, we are able to incorporate complexity into a large number of compounds, increasing our chances of finding a new compound with antimicrobial activity. Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead compounds were systematically modified over four iterations of a Structure Activity Relationship study in an effort to maximize antimicrobial activity. Antimicrobial activity of the compounds from the SAR study against Bacillus subtilis was increased nearly 200-fold from the initial leads and spectrum of activity was expanded to include Staphylococcus aureus and Enterococcus faecalis.
Book Synopsis Natural Product Chemistry for Drug Discovery by : Antony D. Buss
Download or read book Natural Product Chemistry for Drug Discovery written by Antony D. Buss and published by Royal Society of Chemistry. This book was released on 2010 with total page 459 pages. Available in PDF, EPUB and Kindle. Book excerpt: This text provides a comprehensive summary of where natural product chemistry is today in drug discovery. It covers emerging technologies and case studies and is a source of up-to-date information on the topical subject of natural products.
Book Synopsis Privileged Scaffolds in Medicinal Chemistry by : Stefan Bräse
Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Book Synopsis Total Synthesis of Natural Products by : Jie Jack Li
Download or read book Total Synthesis of Natural Products written by Jie Jack Li and published by Springer Science & Business Media. This book was released on 2013-03-14 with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt: 'Total Synthesis of Natural Products' is written and edited by some of today's leaders in organic chemistry. Eleven chapters cover a range of natural products, from steroids to alkaloids. Each chapter contains an introduction to the natural product in question, descriptions of its biological and pharmacological properties and outlines of total synthesis procedures already carried out. Particular emphasis is placed on novel methodologies developed by the respective authors and their research groups. This text is ideal for graduate and advanced undergraduate students, as well as organic chemists in academia and industry.
Book Synopsis Handbook of Combinatorial Chemistry by : K. C. Nicolaou
Download or read book Handbook of Combinatorial Chemistry written by K. C. Nicolaou and published by Wiley-VCH. This book was released on 2002-04-29 with total page 652 pages. Available in PDF, EPUB and Kindle. Book excerpt: In two volumes, this comprehensive handbook provides coverage of the whole area of combinatorial synthetic chemistry, including compound library design and synthesis.
Book Synopsis The Role of Natural Products in Drug Discovery by : J. Mulzer
Download or read book The Role of Natural Products in Drug Discovery written by J. Mulzer and published by Springer Science & Business Media. This book was released on 2013-04-17 with total page 363 pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural Products have been important sources of useful drugs from prehistoric times to the present. This book gives an overview about this field and provides important recent contributions to the discovery of new drugs generated by research on natural products. Total synthesis of natural products with interesting biological activities is paving the way for the preparation of new and improved analogs. The methods of combinatorial chemistry permit the selection of the best drug from a large number of candidates. Beyond synthesis and evaluation of organic molecules a number of new bioorganic methods are coming to the fore and will be discucced in this isue of the ERnst schering Research Foundation workshop proceedings.
Book Synopsis Solid-Phase Synthesis and Combinatorial Technologies by : Pierfausto Seneci
Download or read book Solid-Phase Synthesis and Combinatorial Technologies written by Pierfausto Seneci and published by John Wiley & Sons. This book was released on 2003-05-28 with total page 653 pages. Available in PDF, EPUB and Kindle. Book excerpt: A unique, integrated look at solid-phase synthesis and advances in combinatorial chemistry and technologies The last decade has seen a rapid expansion in combinatorial technologies, a field where chemistry disciplines intersect with automation, statistics, and information science, as well as certain biological disciplines. Reflecting these multidisciplinary trends, this new work provides a comprehensive overview of the most important aspects of solid-phase synthesis (SPS), combinatorial chemistry, and related combinatorial technologies. It clearly demonstrates how SPS and combinatorial chemistry have extended their application from the pharmaceutical arena to new areas, including biotechnology, material sciences, catalysis, and agrochemical industries, and explores in detail strategies for planning, designing, preparing, and testing of combinatorial libraries in various disciplines. Designed to meet the needs of both experienced combinatorial chemists and newcomers to the field, Solid-Phase Synthesis and Combinatorial Technologies: * Surveys the most recent developments in SPS and combinatorial chemistry * Explains the entire process, from determining the need for a library to the details necessary for synthesis of the library * Discusses choice of format, size, and the rationale behind the design of each synthetic step * Surveys the analytical techniques and the purification methods used to characterize and purify combinatorial libraries * Employs a large number of examples to illustrate important concepts * Includes problems geared toward applying acquired knowledge and designing the steps to SPS/library synthesis * Describes the quality control and activity screening of combinatorial libraries for various applications * Features a detailed bibliography of more than 1,700 relevant sources
Book Synopsis Modern Methods of Drug Discovery by : Alexander Hillisch
Download or read book Modern Methods of Drug Discovery written by Alexander Hillisch and published by Birkhäuser. This book was released on 2012-11-28 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt: Research in the pharmaceutical industry today is in many respects quite different from what it used to be only fifteen years ago. There have been dramatic changes in approaches for identifying new chemical entities with a desired biological activity. While chemical modification of existing leads was the most important approach in the 1970s and 1980s, high-throughput screening and structure-based design are now major players among a multitude of methods used in drug discov ery. Quite often, companies favor one of these relatively new approaches over the other, e.g., screening over rational design, or vice versa, but we believe that an intelligent and concerted use of several or all methods currently available to drug discovery will be more successful in the medium term. What has changed most significantly in the past few years is the time available for identifying new chemical entities. Because of the high costs of drug discovery projects, pressure for maximum success in the shortest possible time is higher than ever. In addition, the multidisciplinary character of the field is much more pronounced today than it used to be. As a consequence, researchers and project managers in the pharmaceutical industry should have a solid knowledge of the more important methods available to drug discovery, because it is the rapidly and intelligently combined use of these which will determine the success or failure of preclinical projects.
