| Author | : Armen M. Boldi |
| Publisher | : CRC Press |
| Total Pages | : 363 |
| Release | : 2006-05-16 |
| Genre | : Science |
| ISBN | : 1420009273 |
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
| Author | : Lisa B. English |
| Publisher | : Springer Science & Business Media |
| Total Pages | : 380 |
| Release | : 2008-02-04 |
| Genre | : Science |
| ISBN | : 1592592856 |
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 | : Andrea Trabocchi |
| Publisher | : John Wiley & Sons |
| Total Pages | : 550 |
| Release | : 2013-06-17 |
| Genre | : Science |
| ISBN | : 1118618149 |
Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.
| Author | : K. C. Nicolaou |
| Publisher | : John Wiley & Sons |
| Total Pages | : 826 |
| Release | : 1996-04-11 |
| Genre | : Science |
| ISBN | : 3527292314 |
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.
| Author | : Armen M. Boldi |
| Publisher | : CRC Press |
| Total Pages | : 354 |
| Release | : 2006-05-16 |
| Genre | : Science |
| ISBN | : 1000612015 |
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
| Author | : Stanislav Miertus |
| Publisher | : CRC Press |
| Total Pages | : 597 |
| Release | : 2005-04-12 |
| Genre | : Medical |
| ISBN | : 1420027840 |
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
| Author | : Stephen R. Wilson |
| Publisher | : John Wiley & Sons |
| Total Pages | : 288 |
| Release | : 1997-03-28 |
| Genre | : Medical |
| ISBN | : 9780471126874 |
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.
| Author | : Lixin Zhang |
| Publisher | : Springer Science & Business Media |
| Total Pages | : 380 |
| Release | : 2007-11-17 |
| Genre | : Medical |
| ISBN | : 1592599761 |
A fresh examination of the past successes of natural products as medicines and their new future from both conventional and new technologies. High-performance liquid chromatography profiling, combinatorial synthesis, genomics, proteomics, DNA shuffling, bioinformatics, and genetic manipulation all now make it possible to rapidly evaluate the activities of extracts as well as purified components derived from microbes, plants, and marine organisms. The authors apply these methods to new natural product drug discoveries, to microbial diversity, to specific groups of products (Chinese herbal drugs, antitumor drugs from microbes and plants, terpenoids, and arsenic compounds), and to specific sources (the sea, rainforest, and endophytes). These new opportunities show how research and development trends in the pharmaceutical industry can advance to include both synthetic compounds and natural products, and how this paradigm shift can be more productive and efficacious.
| Author | : Antony D. Buss |
| Publisher | : Royal Society of Chemistry |
| Total Pages | : 459 |
| Release | : 2010 |
| Genre | : Medical |
| ISBN | : 0854041931 |
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.
