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Author: Lisa B. English Publisher: Springer Science & Business Media ISBN: 1592592856 Category : Science Languages : en Pages : 380
Book Description
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.
Author: Lisa B. English Publisher: Springer Science & Business Media ISBN: 1592592856 Category : Science Languages : en Pages : 380
Book Description
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.
Author: Peter Scott Publisher: John Wiley & Sons ISBN: 9780470749050 Category : Science Languages : en Pages : 706
Book Description
Linker design is an expanding field with an exciting future in state-of-the-art organic synthesis. Ever-increasing numbers of ambitious solution phase reactions are being adapted for solid-phase organic chemistry and to accommodate them, large numbers of sophisticated linker units have been developed and are now routinely employed in solid-phase synthesis. Linker Strategies in Solid-Phase Organic Synthesis guides the reader through the evolution of linker units from their genesis in solid-supported peptide chemistry to the cutting edge diversity linker units that are defining a new era of solid phase synthesis. Individual linker classes are covered in easy to follow chapters written by international experts in their respective fields and offer a comprehensive guide to linker technology whilst simultaneously serving as a handbook of synthetic transformations now possible on solid supports. Topics include: the principles of solid phase organic synthesis electrophile and nucleophile cleavable linker units cyclative cleavage as a solid phase strategy photocleavable linker units safety-catch linker units enzyme cleavable linker units T1 and T2 –versatile triazene linker groups hydrazone linker units benzotriazole linker units phosphorus linker units sulfur linker units selenium and tellurium linker units sulfur, oxygen and selenium linker units cleaved by radical processes silicon and germanium linker units boron and stannane linker units bismuth linker units transition metal carbonyl linker units linkers releasing olefins or cycloolefins by ring-closing metathesis fluorous linker units solid-phase radiochemistry The book concludes with extensive linker selection tables, cataloguing the linker units described in this book according to the substrate liberated upon cleavage and conditions used to achieve such cleavage, enabling readers to choose the right linker unit for their synthesis. Linker Strategies in Solid-Phase Organic Synthesis is an essential guide to the diversity of linker units for organic chemists in academia and industry working in the broad areas of solid-phase organic synthesis and diversity oriented synthesis, medicinal chemists in the pharmaceutical industry who routinely employ solid-phase chemistry in the drug discovery business, and advanced undergraduates, postgraduates, and organic chemists with an interest in leading-edge developments in their field.
Author: Patrick H. Toy Publisher: John Wiley & Sons ISBN: 1118141636 Category : Science Languages : en Pages : 560
Book Description
Presents both the fundamental concepts and the most recent applications in solid-phase organic synthesis With its emphasis on basic concepts, Solid-Phase Organic Synthesis guides readers through all the steps needed to design and perform successful solid-phase organic syntheses. The authors focus on the fundamentals of heterogeneous supports in the synthesis of organic molecules, explaining the use of a solid material to facilitate organic synthesis. This comprehensive text not only presents the fundamentals, but also reviews the most recent research findings and applications, offering readers everything needed to conduct their own state-of-the-art science experiments. Featuring chapters written by leading researchers in the field, Solid-Phase Organic Synthesis is divided into two parts: Part One, Concepts and Strategies, discusses the linker groups used to attach the synthesis substrate to the solid support, colorimetric tests to identify the presence of functional groups, combinatorial synthesis, and diversity-oriented synthesis. Readers will discover how solid-phase synthesis is currently used to facilitate the discovery of new molecular functionality. The final chapter discusses how using a support can change or increase reaction selectivity. Part Two, Applications, presents examples of the solid-phase synthesis of various classes of organic molecules. Chapters explore general asymmetric synthesis on a support, strategies for heterocyclic synthesis, and synthesis of radioactive organic molecules, dyes, dendrimers, and oligosaccharides. Each chapter ends with a set of conclusions that underscore the key concepts and methods. References in each chapter enable readers to investigate any topic in greater depth. With its presentation of basic concepts as well as recent findings and applications, Solid-Phase Organic Synthesis is the ideal starting point for students and researchers in organic, medicinal, and combinatorial chemistry who want to take full advantage of current solid-phase synthesis techniques.
Author: Gregg B. Fields Publisher: Academic Press ISBN: Category : Medical Languages : en Pages : 828
Book Description
The critically acclaimed laboratory standard for more than forty years, Methods in Enzymology is one of the most highly respected publications in the field of biochemistry. Since 1955, each volumehas been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. More than 275 volumes have been published (all of them still in print) and much of the material is relevant even today-truly an essential publication for researchers in all fields of life sciences. Key Features * Solid-phase peptide synthesis * Applications of peptides for structural and biological studies * Characterization of synthetic peptides
Author: Pierfausto Seneci Publisher: John Wiley & Sons ISBN: 0471460737 Category : Science Languages : en Pages : 653
Book Description
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
Author: Barry A. Bunin Publisher: Elsevier ISBN: 0080542409 Category : Science Languages : en Pages : 341
Book Description
With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. - Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods - Serves as a laboratory manual for bench chemists - Includes a chapter on linkers to assist in choice of linking strategy - Discusses strengths and limitations of the various methods - Contains a structural index showing functional group transformations in solid-phase synthesis
Author: Joost N. H. Reek Publisher: John Wiley & Sons ISBN: 9783527629718 Category : Science Languages : en Pages : 211
Book Description
This long-awaited first book on this exciting new field in organic and supramolecular chemistry explains the fundamentals as well as possible applications of DCC. Authored by the "Who's Who" of DCC it spans the whole range of topics: catalysts, sensors, polymers, ligands, receptors, concluding with a look at future developments and perspectives. All set to become the standard text in the field, this one-stop reference contains everything organic, catalytic, polymer, physical and biochemists need to know.
Author: Serge L. Beaucage Publisher: Current Protocols ISBN: 9780471246626 Category : Science Languages : en Pages :
Book Description
Good methods must be reliable, well-tested, and honed to minimize the time and expense required to achieve the desired results. CPNC provides a continuously growing and evolving set of protocols that allows researchers to benefit from the experience of other researchers around the world. The core manual provides a comprehensive set of protocols that have been compiled, revised, and streamlined over the last 6 years. Quarterly updates provide new protocols in emerging areas of research as well as continued advances and new applications for fundamental methods. The book is designed to grow and change with the field of nucleic acid chemistry. Fundamental nucleoside chemistry methods include sugar-base condensation, phosphorylation, and nucleoside protection. Methods for oligonucleotide synthesis include H-phosphonate and phosphoramidite approaches, solid-phase and solution-phase synthesis, large-scale synthesis, synthesis for modified and unmodified oligonucleotides, conjugation of oligonucleotides, synthesis without base protection, and synthesis on microarrays. More specialized synthetic methods include synthesis of biologically active nucleosides and prodrugs. Purification and characterization methods are detailed. Advanced methods include biophysical analysis, combinatorial methods, and nanotechnology. Each protocol includes rationale for choosing appropriate methods, step-by-step procedures, complete recipes, anticipated results, characterization data, and troubleshooting, as well as background and recommended reading. The level of procedural detail is far beyond that found in the research literature, and tips and comments from authors are geared towards ensuring reliable duplication in the laboratory.
Author: Nicholas K. Terrett Publisher: ISBN: 9780198502197 Category : Combinatorial chemistry Languages : en Pages : 204
Book Description
Combinatorial chemistry, by accelerating the process of chemical synthesis, is having a profound effect on all branches of chemistry, but especially on drug discovery. This informative text explains the origins of combinatorial chemistry and puts the many diverse library methods into context.It explains why some techniques are generally applicable and others are for specialists only. It also focuses on the renaissance of solid phase chemistry and describes the range of available reactions. This is the first single author book in this important, growing field and it describes thebeneficial impact of combinatorial chemistry, especially for the discovery and optimisation of biologically active molecules. This concise and comprehensive overview of combinatorial techniques is an essential text for final year undergraduates, postgraduates, academics and industrialists inchemistry, bio-orgainc chemistry, medicinal chemistry and drug discovery. It provides an accessible introduction to the area for those new to these methods and a valuable reference text to those experienced in this field.
Author: Lisa B. English
Author: Lisa B. English
Author: Peter Scott
Author: Patrick H. Toy
Author: University of Cambridge
Author: Gregg B. Fields
Author: Pierfausto Seneci
Author: Barry A. Bunin
Author: Joost N. H. Reek
Author: Serge L. Beaucage
Author: Nicholas K. Terrett