Synthetic Methods In Drug Discovery
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| Author | : David C Blakemore |
| Publisher | : Royal Society of Chemistry |
| Total Pages | : 474 |
| Release | : 2016-07-15 |
| Genre | : Science |
| ISBN | : 178262208X |
Synthetic Methods in Drug Discovery Volume 1 focusses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.
| Author | : David C. Blakemore |
| Publisher | : Royal Society of Chemistry |
| Total Pages | : 474 |
| Release | : 2016 |
| Genre | : Medical |
| ISBN | : 1849738033 |
The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.
| Author | : David C. Blakemore |
| Publisher | : Royal Society of Chemistry |
| Total Pages | : 536 |
| Release | : 2016 |
| Genre | : Medical |
| ISBN | : 1782627863 |
The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.
| Author | : Daniel Lednicer |
| Publisher | : John Wiley & Sons |
| Total Pages | : 700 |
| Release | : 2009-03-04 |
| Genre | : Science |
| ISBN | : 9780470399590 |
This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.
| Author | : F. Gualtieri |
| Publisher | : Wiley-VCH |
| Total Pages | : 382 |
| Release | : 2000-03-22 |
| Genre | : Medical |
| ISBN | : |
The long-awaited volume on synthetic chemistry in the series "Methods and Principles in Medicinal Chemistry" is now available. In the pharmaceutical industry, computational methods play a major role in the discovery and development of new drugs. Yet, the SYNTHESIS of these compounds still remains the most crucial topic in drug design. Written by an internationally renowned team of authors and editors from academia and industry, this volume describes all recent developments in organic synthetic methodology which are essential for pharmaceutical research. The most modern synthetic developments of pharmacologically interesting compounds (carbohydrates and nucleotides) as well as important synthetic methods such as combinatorial chemistry, solid-phase reactions, bioassisted organic synthesis and asymmetric synthesis are critically discussed. Special emphasis is given to a hands-on practical approach which enables researchers to apply the featured methods immediately to their specific problems. Also, the detailed presentation of the topic and the selection of references will be of help to any researcher working in the laboratory.
| Author | : David C Blakemore |
| Publisher | : Royal Society of Chemistry |
| Total Pages | : 536 |
| Release | : 2016-07-15 |
| Genre | : Science |
| ISBN | : 178262791X |
Building on key reactions presented in Volume 1, Synthetic Methods in Drug Discovery Volume 2 covers a range of important reaction types including organometallic chemistry, fluorination approaches and asymmetric methods as well as new and exciting areas such as Csp2-Csp3 couplings, catalytic amide bond forming reactions, hydrogen borrowing chemistry and methods to access novel motifs and monomers. This book provides both academic and industrial perspectives on key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Moreover, key opportunities in expanding chemical space are presented, including the increasingly important syntheses that introduce three-dimensional molecular shape. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.
| Author | : Andrea Trabocchi |
| Publisher | : Elsevier |
| Total Pages | : 358 |
| Release | : 2019-11-23 |
| Genre | : Science |
| ISBN | : 0128183500 |
Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. - Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery - Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics - Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches - Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules
| Author | : Clay S. Bennett |
| Publisher | : John Wiley & Sons |
| Total Pages | : 398 |
| Release | : 2017-01-25 |
| Genre | : Science |
| ISBN | : 3527696229 |
A comprehensive summary of novel approaches to the stereoselective construction of glycosidic linkages, covering modern glycosylation methods and their use and application in natural product synthesis and drug discovery. Clearly divided into five sections, the first describes recent advances in classical methodologies in carbohydrate chemistry, while the second goes on to deal with newer chemistries developed to control selectivity in glycosylation reactions. Section three is devoted to selective glycosylation reactions that rely on the use of catalytic promoters. Section four describes modern approaches for controlling regioselectivity in carbohydrate synthesis. The final section focuses on new developments in the construction of "unusual" sugars and is rounded off by a presentation of modern procedures for the construction of glycosylated natural products. By providing the latest advances in glycosylation as well as information on mechanistic aspects of the reaction, this is an invaluable reference for both specialists and beginners in this booming interdisciplinary field that includes carbohydrate chemistry, organic synthesis, catalysis, and biochemistry.
| 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 | : S. Grabley |
| Publisher | : Springer Science & Business Media |
| Total Pages | : 380 |
| Release | : 1998-11-26 |
| Genre | : Medical |
| ISBN | : 9783540648444 |
This book is unique in covering the present status and future potential of natural products in drug discovery. It provides readers with recent information regarding the impact on drug discovery, development and strategies, technical and automation aspects, and methods based on biochemistry as well as molecular biology, highlighting compounds from natural sources. Special emphasis is placed on the various strategies to gain access to natural compounds and combinatorial approaches by making use of both synthetic and biological methods.
