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Macrocycles In Drug Discovery
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Book Synopsis Macrocycles in Drug Discovery by : Jeremy I Levin
Download or read book Macrocycles in Drug Discovery written by Jeremy I Levin and published by Royal Society of Chemistry. This book was released on 2015 with total page 526 pages. Available in PDF, EPUB and Kindle. Book excerpt: This series provides a comprehensive resource for postgraduate students and for scientists in academia or industry wanting to learn topics outside their own areas of expertise.
Book Synopsis Macrocycles in Drug Discovery by : Jeremy Levin
Download or read book Macrocycles in Drug Discovery written by Jeremy Levin and published by Royal Society of Chemistry. This book was released on 2014-10-03 with total page 525 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews 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. The medicinal chemistry of macrocyclic natural products is interesting in itself, but lessons learned from these compounds, in terms of the relationship between structure and desirable physicochemical properties, are now informing the design of fully synthetic macrocyclic drug candidates against a variety of targets including kinases, ATPases, proteases, GPCRs and others. Furthermore, as more non-classical drug targets, such as protein–protein interactions, are pursued in the pharmaceutical industry, macrocyclic molecules are generating increasing interest as they offer a way to provide drug–protein interactions that cover a larger surface area than traditional small molecules. A variety of macrocycles have become important drugs or have been identified as leads to marketed drugs. This text will discuss these compounds, their pharmacology and synthesis, in the context of their broad chemotype as compounds composed of large rings. 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.
Book Synopsis Practical Medicinal Chemistry with Macrocycles by : Eric Marsault
Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-09-12 with total page 617 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Small Molecule Drug Discovery by : Andrea Trabocchi
Download or read book Small Molecule Drug Discovery written by Andrea Trabocchi and published by Elsevier. This book was released on 2019-11-23 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Inhibitors of Protein–Protein Interactions by : Ali Tavassoli
Download or read book Inhibitors of Protein–Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis The Practice of Medicinal Chemistry by : Camille Georges Wermuth
Download or read book The Practice of Medicinal Chemistry written by Camille Georges Wermuth and published by Elsevier. This book was released on 2015-07-01 with total page 903 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Diversity Oriented Synthesis by : Andrea Basso
Download or read book Diversity Oriented Synthesis written by Andrea Basso and published by Frontiers Media SA. This book was released on 2019-03-22 with total page 150 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Peptide Macrocycles by : Matthew B. Coppock
Download or read book Peptide Macrocycles written by Matthew B. Coppock and published by Humana. This book was released on 2021-11-02 with total page 469 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Author :Jayaveera K.N./ Subramanyam S. & Reddy, Yogananda K. Publisher :S. Chand Publishing ISBN 13 :8121942454 Total Pages :166 pages Book Rating :4.1/5 (219 download)
Book Synopsis Practical Medicinal Chemistry by : Jayaveera K.N./ Subramanyam S. & Reddy, Yogananda K.
Download or read book Practical Medicinal Chemistry written by Jayaveera K.N./ Subramanyam S. & Reddy, Yogananda K. and published by S. Chand Publishing. This book was released on with total page 166 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introduction 2. Synthesis Of Some Official Medicinal Compounds 3. Assay Of Some Official Compounds 4. Monograph Analysis Of The Following Compounds 5. Identification And Estimation Of Drug Metabolites From Biological Fluids 6. Determination Of Partition Coefficient Of Compounds For Qsar Analysis 7. I.R. Spectra Of Some Official Medicinal Compounds
Book Synopsis Diversity-Oriented Synthesis by : Andrea Trabocchi
Download or read book Diversity-Oriented Synthesis written by Andrea Trabocchi and published by John Wiley & Sons. This book was released on 2013-06-17 with total page 550 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud
Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Book Synopsis Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design by : Sanjeev Kumar Singh
Download or read book Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design written by Sanjeev Kumar Singh and published by Springer Nature. This book was released on 2021-02-02 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents various computer-aided drug discovery methods for the design and development of ligand and structure-based drug molecules. A wide variety of computational approaches are now being used in various stages of drug discovery and development, as well as in clinical studies. Yet, despite the rapid advances in computer software and hardware, combined with the exponential growth in the available biological information, there are many challenges that still need to be addressed, as this book shows. In turn, it shares valuable insights into receptor-ligand interactions in connection with various biological functions and human diseases. The book discusses a wide range of phylogenetic methods and highlights the applications of Molecular Dynamics Simulation in the drug discovery process. It also explores the application of quantum mechanics in order to provide better accuracy when calculating protein-ligand binding interactions and predicting binding affinities. In closing, the book provides illustrative descriptions of major challenges associated with computer-aided drug discovery for the development of therapeutic drugs. Given its scope, it offers a valuable asset for life sciences researchers, medicinal chemists and bioinformaticians looking for the latest information on computer-aided methodologies for drug development, together with their applications in drug discovery.
Book Synopsis Carbohydrates in Drug Discovery and Development by : Vinod K. Tiwari
Download or read book Carbohydrates in Drug Discovery and Development written by Vinod K. Tiwari and published by Elsevier. This book was released on 2020-08-17 with total page 714 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbohydrates in Drug Discovery and Development: Synthesis and Application examines important developments in the synthesis, biology and biomedical applications of carbohydrates, along with the therapeutic and pharmacological aspects of carbohydrate chemistry. In addition to the advancement in construction of oligosaccharides, chemists are also making strides in the ability to assemble glycopeptides and glycoproteins. This book covers advanced aspects of carbohydrates, starting with a brief introduction, nomenclature and classification that is followed by a discussion of glyosidic bond formation methodology, recent protocols for the synthesis of O-glycosides, N-glycosides, thioglycosides and C-glycosides, Intramolecular Aglycon Delivery (IAD), carbohydrate modification, and more. Written by a team of international experts actively working on different aspect of synthetic carbohydrate chemistry, this book is an invaluable resource for carbohydrate chemists, natural products chemists, medicinal chemists, synthetic organic chemists and biochemists working in industry and academia. Gives a practical, detailed overview on a wide range of carbohydrate systems relevant for drug discovery and development Highlights applications of functionalized carbohydrates and their use as synthons for the construction of various systems Covers recent developments in the synthesis of various glycohybrid molecules
Book Synopsis Click Reactions in Organic Synthesis by : Srinivasan Chandrasekaran
Download or read book Click Reactions in Organic Synthesis written by Srinivasan Chandrasekaran and published by John Wiley & Sons. This book was released on 2016-09-13 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: Endlich ein Buch zu Click-Reaktionen mit Schwerpunkt auf der organischen Synthese. Beschrieben werden das Click-Konzept, die zugrunde liegenden Mechanismen und Hauptanwendungsgebiete. NÜTZLICH: Die Click-Chemie ist ein wirkungsvoller Ansatz, um auf einfache Weise komplexe organische Moleküle aus verfügbaren Ausgangsmaterialien zu erzeugen ? der Traum jedes Organikers. EINZIGARTIGER SCHWERPUNKT: Aufgrund des besonderen Schwerpunkts auf der organischen Synthese ist dieses Buch für jeden Synthesechemiker von hohem Interesse. HILFREICH: Click-Reaktionen sind stereospezifisch, einfach durchzuführen, hoch ergiebig und lassen sich in einfach zu entfernenden oder nicht schädlichen Lösungsmitteln durchführen. INTERDISZIPLINÄR: Das Click-Konzept ist bei der Herstellung natürlicher Produkte, bioaktiver Verbindungen, von Kohlenhydraten, Arzneimitteln, Polymeren, supramolekularer Strukturen und Materialien weit verbreitet.
Book Synopsis Multicomponent Reactions towards Heterocycles by : Erik Van der Eycken
Download or read book Multicomponent Reactions towards Heterocycles written by Erik Van der Eycken and published by John Wiley & Sons. This book was released on 2022-03-21 with total page 626 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Supramolecular Systems in Biomedical Fields by : Hans-Jorg Schneider
Download or read book Supramolecular Systems in Biomedical Fields written by Hans-Jorg Schneider and published by Royal Society of Chemistry. This book was released on 2013-09-06 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: Non-covalent interactions, which are the heart of supramolecular chemistry are also the basis of most important functions of living systems. The ability to apply supramolecular chemistry principles to the life sciences, such as designing synthetic host compounds to selectively interact within biological targets, has gained wide appeal due the vast number of potential applications. Supramolecular Systems for Biomedical Fields provides in sixteen chapters a comprehensive overview of these applications. Each chapter covers a specific topic and is written by internationally renowned experts in that area. Sensing of bioactive inorganic ions and organic substrates is the focus of several contributions, as well as interactions with proteins and nucleic acids. Specific chapters are devoted to cyclodextrins, calixarenes and cucurbiturils as most frequently used receptors, including applications such as drug delivery and protection, gene transfer and others. Other chapters address the use of combinatorial libraries, molecular imprinting techniques, enzyme assays, supramolecular gels, bioimaging, drug activation, photodynamic therapy, and antitumour metal complexes. This timely publication will appeal to graduate students and researchers from chemical, pharmaceutical, biological, and medicinal fields interested in the supramolecular chemistry of biological systems and their practical potentials.
Book Synopsis Applications of Transition Metal Catalysis in Drug Discovery and Development by : Matthew L. Crawley
Download or read book Applications of Transition Metal Catalysis in Drug Discovery and Development written by Matthew L. Crawley and published by John Wiley & Sons. This book was released on 2012-05-14 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book focuses on the drug discovery and development applications of transition metal catalyzed processes, which can efficiently create preclinical and clinical drug candidates as well as marketed drugs. The authors pay particular attention to the challenges of transitioning academically-developed reactions into scalable industrial processes. Additionally, the book lays the groundwork for how continued development of transition metal catalyzed processes can deliver new drug candidates. This work provides a unique perspective on the applications of transition metal catalysis in drug discovery and development – it is a guide, a historical prospective, a practical compendium, and a source of future direction for the field.
