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Combinatorial chemistry has taken the pharmaceutical industry by storm over the past ten to fifteen years. There has been a massive investment in automation by pharmaceutical companies and a demand for graduates/PhDs with experience and knowledge of combinatorial chemistry. These days the academic education of chemists and biologists is gradually converging, so those entering the pharmaceutical industry need to be not only chemistry graduates but also biologists applying their biological knowledge to chemistry. Many chemists, however, still require experience in biological methods and similarly biologists have not yet realized the power of chemical methods. This book will therefore help ease the transition from biology into chemistry and vice versa, for those working in the combinatorial chemistry field. Because combinatorial chemistry evolved from the requirements of the biology field, the authors have written this book with both biologists and chemists in mind. Combinatorial chemistry is a new and highly influential area of modern synthetic chemistry based on efficient, parallel synthesis of molecules, as opposed to the use of several synthetic steps, to produce many sets of compounds for biological evaluation. The techniques used in this area are key to the discovery of new drug compounds in the pharmaceutical and agrochemical industries. Combinatorial Methods in Chemistry and Biology describes the origins, basics and techniques used both in combinatorial chemistry and molecular biology. Key features: * First book to cover combinatorial methods in both chemistry and biology - ideal for those with either a chemical or biological background. * Introductory text - ideal for newcomers to the field. * Covers a wide swathe of techniques and topics - providing beginners with a complete overview of the field. * Contains chapters on supporting material and linkers, two important areas in the field. * Up-to-date and topical. This volume will be of key interest to technicians/scientists working in the pharmaceutical industry with backgrounds in either biology or chemistry. It will also be invaluable to students - postgraduates studying chemistry and molecular biology or those chemistry/molecular biology undergraduates at universities where combinatorial chemistry is taught as a module.
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.
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.
The essence of combinatorial chemistry or techniques involving "molecular diversity" is to generate enormous populations of molecules and to exploit appropriate screening techniques to isolate active components contained in these libraries. This idea has been the focus of research both in academia and in the pharmaceutical or biotechnology industry. Its developments go hand in hand with an exploding number of potential drug targets emerging from genomics and proteomics research. When the editors of Current Topics in Microbiology and Immunology encouraged us to assemble the present volume on Combinatorial Chemistry in Biology, we immediately felt that this might prove quite beneficial for the audience of this series. The field of combinatorial chemistry extends over a broad range of disciplines, from synthetic organic chemistry to biochemistry, from material sciences to cell biology. Each of these fields may have its own view on this topic, something which is reflected in a growing number of monographs and "special editions" of jour nals devoted to this issue or aspects thereof. The title of the present volume of Springer-Verlag's series suggests that it also has its own special focus. And, generally speaking, this is not wrong: we would even claim the special focus of this volume is on the immunologically relevant aspects of combinatorial chemistry.
Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. - New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations - Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years - Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization
Unparalleled in size and scope, this new major reference integrates academic and industrial knowledge into a single resource, allowing for a unique overview of the entire field. Adopting a systematic and practice-oriented approach, and including a wide range of technical and methodological information, this highly accessible handbook is an invaluable 'toolbox' for any bioengineer. In two massive volumes, it covers the full spectrum of current concepts, methods and application areas.
In two volumes, this comprehensive handbook provides coverage of the whole area of combinatorial synthetic chemistry, including compound library design and synthesis.
The newer research areas in pharmaceutical sciences, particularly molecular modeling and simulations, prompted a more efficient drug discovery process. Informatics integrated with pharmaceutical sciences (cheminformatics and bioinformatics) became an essential component of drug research. Drug informatics such as genomics and proteomics assists in the Rational Drug Design (RDD). This emerging discipline is known as “Computer-Aided Drug Design (CADD)”, which has profound application in rational drug design (RDD). The advanced and adequate practice in drug design informatics is essential for pharmacy graduates. Hence, a companion for acquiring knowledge on these concepts is vital. The students of B. Pharmacy, M. Pharmacy (Pharmaceutical Chemistry, Pharmacology, and Pharmaceutics), biotechnology, biomedical engineering and other interdisciplinary fields may find this book as a reference guide. The salient features of this book are: • Systematic and simple approach • Emphasis on traditional and modern drug design strategies • Comprehensive coverage for the current advances in the drug design • Experimental section to ensure hands-on-experience Note: T& F does not sell or distribute the Hardback in India, Pakistan, Nepal, Bhutan, Bangladesh and Sri Lanka.
Synthetic chemistry plays a central role in many areas of chemical biology; utilising recent case studies, the goal of Chemical and Biological Synthesis is to highlight the full impact that the preparation of novel reagents can have in chemical biology. Covering the synthetic approaches that can be applied across the whole field of chemical biology, this book provides synthetic chemists with the broader context to which their work contributes and the biological questions that can be addressed through it. An ideal guide for postgraduate students and researchers in synthetic organic chemistry and chemical biology, Chemical and Biological Synthesis introduces synthetic techniques and methods to those who wish to incorporate synthesis for the first time in their biology-focused research programmes.
This is a fascinating introduction to the topic. Spanning the spectrum of nucleic acid chemistry, carbohydrates, peptides, molecular recognition, biosynthesis and natural biosynthesis, right up to medical and biophysical chemistry, the book provides advanced students and those already working in the field with a balanced overview. In more than 30 contributions, a new generation of recognized scientists gives an account of the latest research in such areas as * Artificial receptors for the stabilization of ß-sheet structures * Carbohydrate recognition by artificial receptors * Combinatorial chemistry as a tool for the discovery of catalysts * The interaction of NO and peroxynitrite with hemoglobin and myoglobin * Inhibitors against human mast-cell-tryptase as a potential approach to conquering asthma * The selectivity of DNA replication. A readily accessible survey for everyone wishing to stay abreast of developments. With a Foreword by Ronald Breslow.