Optimization of Solid-Phase Combinatorial Synthesis


Book Description

"Addresses the key topic in combinatorial synthesis--how to optimize the quality of a combinatorial library--by determining the usefulness of synthesized compunds, the reliability of biological assay results, and analyzing acadmic and industrial applications, real-world examples, and case studies of successful and unsuccessful technologies."




Solid-Phase Synthesis and Combinatorial Technologies


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




Handbook of Combinatorial Chemistry


Book Description

In two volumes, this comprehensive handbook provides coverage of the whole area of combinatorial synthetic chemistry, including compound library design and synthesis.




Small Molecule — Protein Interactions


Book Description

Based on the international workshop on 'Small Molecule - Protein Interactions' held in Berlin, April 24-26, 2002, researchers from industry and academic laboratories describe novel and efficient ways selecting promising new drug targets and developing small molecule inhibitors against them. The structure of the book corresponds to the different aspects of the drug discovery process. All chapters are written by leading experts in the field, who present and discuss the most recent state-of-the-art tools and techniques for the development of novel drugs. The value of the book lies in surveying and summarizing the approaches taken by different companies and institutions giving the reader a balanced view on the use of the latest techniques on the one hand and experience-based assistance in selecting appropriate tools for their own work on the other hand.




Combinatorial Library


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.




High-Throughput Lead Optimization in Drug Discovery


Book Description

A Single Source on Parallel Synthesis for Lead Optimization The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high qualit




Combinatorial Chemistry and Technologies


Book Description

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




Combinatorial Chemistry


Book Description

Combinatorial Chemistry is a genuine practical guide covering all the major areas of combinatorial chemistry from an experimental and conceptual point of view. Being one of the most powerful of modern technologies, combinatorial chemistry has had implications to many areas of chemistry and biology and the current approaches to drug, catalyst, receptor, and materials development and discovery are all included in this volume. It also contains protocols on solid, liquid, and solution phase synthesis and expedient methods of library screening and evaluation. The use of automation and robotics is also explained. It is written at a level easily accessible to novices and will enable readers to use combinatorial techniques to the best advantage.




High-Throughput Analysis in the Pharmaceutical Industry


Book Description

The introduction of combinatorial chemistry technology has increased the amount of compounds generated in a year from 50 to 2000. Conventional analytical approaches simply cannot keep up. These circumstances have caused drug discovery to take on the shape of a bottleneck, like traffic through a toll booth. In order to break the bottleneck, a corres




Green Approaches in Medicinal Chemistry for Sustainable Drug Design


Book Description

Extensive experimentation and high failure rates are a well-recognised downside to the drug discovery process, with the resultant high levels of inefficiency and waste producing a negative environmental impact. Sustainable and Green Approaches in Medicinal Chemistry, Second Edition reveals how medicinal chemistry can play a direct role in addressing this issue. After providing essential context to the growth of green chemistry in relation to drug discovery, the book goes on to identify a broad range of practical techniques and useful insights, revealing how medicinal chemistry techniques can be used to improve efficiency, mitigate failure and increase the environmental benignity of the entire drug discovery process. Drawing on the knowledge of a global team of experts, Sustainable and Green Approaches in Medicinal Chemistry 2e encourages the growth of green medicinal chemistry, and supports medicinal chemists, drug discovery researchers, pharmacologists and all those in related fields across both academia and industry in integrating these approaches into their own work. This first volume of the second edition covers synthesis methods following green chemistry principles, contributing to sustainability by saving energy, using lesser toxic reagents/solvents/catalysts and environmentally benign sources including plants and agricultural materials. - Highlights the need for the adoption of sustainable and green chemistry pathways in drug development - Reveals risk factors associated with the drug development process and the ways sustainable approaches can help address these factors - Identifies novel and cost effective green medicinal chemistry approaches for improved efficiency and sustainability