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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
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.
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
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 methodologies used in the design, synthesis, and screening of molecular libraries. Now in its second edition, this volume updates prior content and explores new areas such as catalysis, applications in biotechnology, and current ICS-UNIDO activities. Topics include the generation of molecular diversity by chemical methods using solution- and solid-phase chemistries, biological approaches for the production and screening of peptides, antibody and oligonucleotide libraries, and the application of computer-assisted approaches to guide library synthesis. The book establishes the link between combinatorial chemistry and molecular modeling and illustrates the importance of economics and patenting in combinatorial technologies. Valuable to technologists and researchers as an introductory survey on the many aspects of combinatorial chemistry and combinatorial technology, Combinatorial Chemistry and Technologies: Methods and Applications offers an overview of a field that promises broad applicability in the identification of new drugs, as well as in diagnostics, new materials, and catalysis.
"Provides comprehensive coverage of the current combinatorial methodologies and technologies employed for the design, synthesis, and screening of molecular ""libraries."" Features assessments of computer-assisted approaches to guiding library synthesis. Designed to satisfy the demand to create, produce in high yield and purity, and rapidly screen huge numbers of molecules."
In two volumes, this comprehensive handbook provides coverage of the whole area of combinatorial synthetic chemistry, including compound library design and synthesis.
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.
This book comprehensively describes the development and practice of DNA-encoded library synthesis technology. Together, the chapters detail an approach to drug discovery that offers an attractive addition to the portfolio of existing hit generation technologies such as high-throughput screening, structure-based drug discovery and fragment-based screening. The book: Provides a valuable guide for understanding and applying DNA-encoded combinatorial chemistry Helps chemists generate and screen novel chemical libraries of large size and quality Bridges interdisciplinary areas of DNA-encoded combinatorial chemistry – synthetic and analytical chemistry, molecular biology, informatics, and biochemistry Shows medicinal and pharmaceutical chemists how to efficiently broaden available "chemical space" for drug discovery Provides expert and up-to-date summary of reported literature for DNA-encoded and DNA-directed chemistry technology and methods
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.
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