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Diversity-Oriented Synthesis

Author: Andrea Trabocchi

Publisher: John Wiley & Sons

Published: 2013-06-17

Total Pages: 550

ISBN-13: 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.

Diversity Oriented Synthesis

Author: Andrea Basso

Publisher: Frontiers Media SA

Published: 2019-03-22

Total Pages: 150

ISBN-13: 2889457885

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Has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade.

Fragment-based Approaches in Drug Discovery

Author: Wolfgang Jahnke

Publisher: John Wiley & Sons

Published: 2006-12-13

Total Pages: 391

ISBN-13: 3527608605

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This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.

The Ionotropic Glutamate Receptors

Author: Daniel Monaghan

Publisher: Springer Science & Business Media

Published: 2012-12-06

Total Pages: 381

ISBN-13: 1461239621

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The Ionotropic Glutamate Receptors provides the first detailed survey of the biochemical, physiological, and pharmacological properties of recombinant ionotropic glutamate receptors. The distinguished contributors show how the molecular characteristics of these receptors account for many of the properties of native ionotropic glutamate receptors. They also examine in detail the properties of glutamate receptor subunits, including receptor modulation by phosphorylation and the anatomical localization of specific glutamate receptor subunits as determined by in situ hybridization and immunochemistry. The Ionotropic Glutamate Receptors conveys the first clear insights into the molecular bases underlying the wealth of pharmacological and physiological data on these receptors.

Natural Product Synthesis I

Author: Johann H. Mulzer

Publisher: Springer Science & Business Media

Published: 2005-01-12

Total Pages: 258

ISBN-13: 9783540211259

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B. Basler, S. Brandes, A. Spiegel and T. Bach: Total Synthesis of Kalsoene and Preussin .- R. Bandichhor, B. Nosse and O. Reiser: Paraconic Acids- the Natural Products from Lichen Symbiont .- M. Hiersemann and H. Helmboldt: Recent Progress in the Total Synthesis of Dolabellane and Dolastane Diterpenes .- L. Wessjohann and E. Ruijter: Strategies for Total and Diversity- Oriented Synthesis of Natural Product (-Like) Macrolides .-M. Sefkow: Enantioselectice Synthesis of C(8)-Hydroxylated Lignans: Early Approaches and Recent Advances

Chemical and Biological Synthesis

Author: Nick J Westwood

Publisher: Royal Society of Chemistry

Published: 2018-08-16

Total Pages: 339

ISBN-13: 178801507X

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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.

Multicomponent Reactions towards Heterocycles

Author: Erik Van der Eycken

Publisher: John Wiley & Sons

Published: 2022-03-21

Total Pages: 626

ISBN-13: 3527349081

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Presents a wide-ranging overview of essential topics and recent advances in MCR chemistry Heterocycles are a central component in natural product chemistry, pharmaceuticals, agrochemicals, and material science. New synthetic methodologies integrating the sequencing of multicomponent reactions (MCRs) are today being used for the rapid synthesis of diversified heterocycles in just one step. Multicomponent Reactions towards Heterocycles presents an up-to-date summary MCR chemistry with a focus on the conjugation between modern synthetic methodologies and MCRs. Featuring contributions by leaders in the field, this comprehensive resource highlights applications of MCRs in natural products and intermediate synthesis, discusses current trends and future prospects in MCR chemistry, outlines novel multicomponent procedures, and more. The authors provide the practical information required for designing new reaction strategies and mechanisms, covering topics including MCR-based green synthetic methods, cyclization and cycloaddition reactions, heterocycle multicomponent syntheses in a continuous flow, catalytic alkynoyl generation, MCR synthesis of saturated heterocycles, and C–H functionalization and multicomponent reactions. Provides a thorough overview of heterocycles as input in multicomponent reactions Discusses recent advances in the field of MCR chemistry and progress in the synthesis and functionalization of heterocycles Demonstrates the use of MCRs to simplify synthetic design and achieve complexity and diversity in novel bioactive molecules Highlights examples of multicomponent polymerizations, target-oriented synthesis, and applications of MCR in medicinal chemistry Explains the methodology of using on-resin MCRs to produce heterocycle compounds Illustrating the key role of MCRs towards heterocycles in natural product synthesis, drug discovery, organic synthesis, and other applications, Multicomponent Reactions towards Heterocycles is required reading for synthetic chemists in academia and industry alike.

Practical Medicinal Chemistry with Macrocycles

Author: Eric Marsault

Publisher: John Wiley & Sons

Published: 2017-09-12

Total Pages: 617

ISBN-13: 1119092566

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Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations

Small Molecule Medicinal Chemistry

Author: Werngard Czechtizky

Publisher: John Wiley & Sons

Published: 2015-09-25

Total Pages: 528

ISBN-13: 1118771699

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Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting

Functional Organic Materials

Author: Thomas J. J. Müller

Publisher: John Wiley & Sons

Published: 2007-02-12

Total Pages: 622

ISBN-13: 9783527313020

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This timely overview of the syntheses for functional pi-systems focuses on target molecules that have shown interesting properties as materials or models in physics, biology and chemistry. The unique concept allows readers to select the right synthetic strategy for success, making it invaluable for a number of industrial applications. A "must have" for everyone working in this new and rapidly expanding field.