Macrocycles In Drug Discovery
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Practical Medicinal Chemistry With Macrocycles
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Author : Eric Marsault
language : en
Publisher: John Wiley & Sons
Release Date : 2017-08-04
Practical Medicinal Chemistry With Macrocycles written by Eric Marsault and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-08-04 with Science categories.
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
Macrocycles In Drug Discovery
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Author : Jeremy I Levin
language : en
Publisher: Royal Society of Chemistry
Release Date : 2015
Macrocycles In Drug Discovery written by Jeremy I Levin and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015 with Medical categories.
This book will review macrocycles in drug discovery, both those of natural origin and semi-synthetic derivatives of natural products, and those designed and synthesized based on principles of medicinal chemistry. A variety of macrocyclic natural products have become important drugs or have been identified as leads to marketed drugs. This text will discuss these compounds in the context of their broad chemotype as compounds composed of large rings. The medicinal chemistry of natural products is interesting in itself, but lessons learned from these compounds, in terms of the relationship between structure and desirable physicochemical properties, is now informing the design of fully synthetic drug candidates against a variety of targets. Furthermore, as more and more non-classical drug targets, such as protein-protein interactions, are pursued in the pharmaceutical industry, macrocyclic molecules are becoming increasingly important as they offer a way to provide drug-protein interactions that cover a larger surface area than traditional small molecules. An indication of this growing importance is the fact that several companies now provide libraries of macrocyclic molecules produced by proprietary chemical technology to use for lead generation. Providing a wide reaching review of this important area in a single volume, this book will be of interest to biochemists, pharmaceutical scientists and medicinal chemists working in industry or academia.
Small Molecule Drug Discovery
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Author : Andrea Trabocchi
language : en
Publisher: Elsevier
Release Date : 2019-11-23
Small Molecule Drug Discovery written by Andrea Trabocchi and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-11-23 with Science categories.
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
Cucurbiturils And Related Macrocycles
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Author : Kimoon Kim
language : en
Publisher: Royal Society of Chemistry
Release Date : 2019-11-06
Cucurbiturils And Related Macrocycles written by Kimoon Kim and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-11-06 with Science categories.
This book provides a complete overview of cucurbituril chemistry, covering fundamental aspects including history, synthesis and host-guest chemistry.
The Practice Of Medicinal Chemistry
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Author : Camille Georges Wermuth
language : en
Publisher: Elsevier
Release Date : 2015-07-01
The Practice Of Medicinal Chemistry written by Camille Georges Wermuth and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-07-01 with Science categories.
The Practice of Medicinal Chemistry, Fourth Edition provides a practical and comprehensive overview of the daily issues facing pharmaceutical researchers and chemists. In addition to its thorough treatment of basic medicinal chemistry principles, this updated edition has been revised to provide new and expanded coverage of the latest technologies and approaches in drug discovery. With topics like high content screening, scoring, docking, binding free energy calculations, polypharmacology, QSAR, chemical collections and databases, and much more, this book is the go-to reference for all academic and pharmaceutical researchers who need a complete understanding of medicinal chemistry and its application to drug discovery and development. Includes updated and expanded material on systems biology, chemogenomics, computer-aided drug design, and other important recent advances in the field Incorporates extensive color figures, case studies, and practical examples to help users gain a further understanding of key concepts Provides high-quality content in a comprehensive manner, including contributions from international chapter authors to illustrate the global nature of medicinal chemistry and drug development research An image bank is available for instructors at www.textbooks.elsevier.com
Carbohydrates In Drug Discovery And Development
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Author : Vinod K. Tiwari
language : en
Publisher: Elsevier
Release Date : 2020-07-31
Carbohydrates In Drug Discovery And Development written by Vinod K. Tiwari and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2020-07-31 with Science categories.
Carbohydrates in Drug Discovery and Development: Synthesis and Applications examines recent and notable developments in the synthesis, biology, therapeutic, and biomedical applications of carbohydrates, which is considered to be a highly promising area of research in the field of medicinal chemistry. Their role in several important biological processes, notably energy storage, transport, modulation of protein function, intercellular adhesion, malignant transformation, signal transduction, viral, and bacterial cell surface recognition formulate the carbohydrate systems to be an exceedingly considerable scaffold for the development of new chemical entities of pharmacological importance. In addition to their easy accessibility, high functionality and chiralpool characteristics are the few additional fascinating structural features of carbohydrates, which further enhance their utilities and thus they have been able to attract chemists and biologists toward harnessing these properties for the past several decades. This book covers an advanced aspect of carbohydrate-based molecular scaffolding, starting with a general introduction followed by a detailed discussion about the impact of diverse carbohydrate-containing molecules of great therapeutic values and their impact on drug discovery and development. The topics covered in this book include the significance of heparin mimetics as the possible tools for the modulation of biology and therapy, chemistry and bioactivities of C-glycosylated compounds, inositols, iminosugars, KDO, sialic acids, glycohybrids, macrocycles, plant oligosaccharides, anti-bacterial and anti-cancer vaccines, antibiotics, and more. • Presents a practical and detailed overview of a wide range of carbohydrate systems including KDO, sialic acids, inositols, iminosugars, etc relevant for drug discovery and development. • Highlights the use of functionalized carbohydrates as synthons for the construction of various systems. • Covers recent developments in the synthesis of various glycohybrid molecules and vaccines. • Highlights the significance of heparin mimetics as tools for the modulation of biology. • Provides an impact of glycan microarrays and carbohydrate– protein interaction.
Synthesis Of Heterocycles Via Multicomponent Reactions Ii
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Author : Romano V. A. Orru
language : en
Publisher: Springer
Release Date : 2010-07-26
Synthesis Of Heterocycles Via Multicomponent Reactions Ii written by Romano V. A. Orru and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-07-26 with Science categories.
Géraldine Masson, Luc Neuville ∙ Carine Bughin ∙ Aude Fayol ∙ Jieping Zhu Multicomponent Syntheses of Macrocycles Thomas J.J. Müller Palladium-Copper Catalyzed Alkyne Activation as an Entry to Multicomponent Syntheses of Heterocycles Rachel Scheffelaar ∙ Eelco Ruijter ∙ Romano V.A. Orru Multicomponent Reaction Design Strategies: Towards Scaffold and Stereochemical Diversity Nicola Kielland ∙ Rodolfo Lavilla Recent Developments in Reissert-Type Multicomponent Reactions Jitender B. Bariwal ∙ Jalpa C. Trivedi ∙ Erik V. Van der Eycken Microwave Irradiation and Multicomponent Reactions Irini Akritopoulou-Zanze ∙ Stevan W. Djuric Applications of MCR-Derived Heterocycles in Drug Discovery
Cyclic Peptide Design
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Author : Gilles Goetz
language : en
Publisher: Methods in Molecular Biology
Release Date : 2020-06-11
Cyclic Peptide Design written by Gilles Goetz and has been published by Methods in Molecular Biology this book supported file pdf, txt, epub, kindle and other format this book has been release on 2020-06-11 with Medical categories.
Inhibitors Of Protein Protein Interactions
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Author : Ali Tavassoli
language : en
Publisher: Royal Society of Chemistry
Release Date : 2020-12-07
Inhibitors Of Protein Protein Interactions written by Ali Tavassoli and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2020-12-07 with Science categories.
Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.
Peptide Macrocycles
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Author : Matthew B. Coppock
language : en
Publisher: Humana
Release Date : 2021-11-02
Peptide Macrocycles written by Matthew B. Coppock and has been published by Humana this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-11-02 with Technology & Engineering categories.
This volume explores the latest techniques and strategies used to study the field of peptide macrocycles. The chapters in this book ae organized into four parts: macrocycles synthesis, combinational library synthesis and screening, macrocycle characterization, and unique applications. Part One looks at a variety of peptide cyclization methodologies, and Part Two describes methods for the creation of peptide macrocycles libraries and their subsequent screening against biological targets of interest. Part Three discusses the study and characterization of peptide macrocycle-target interactions, and Part Four introduces unique applications for peptide macrocycles, from higher-order structure formation to post-synthetic functional modifications. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and comprehensive, Peptide Macrocycles: Methods and Protocols is a valuable resource for both novice and expert researchers looking to learn more about this developing field.