Medicinal Chemistry and Synthesis

Author: Larry Yet

Publisher: John Wiley & Sons

ISBN: 1118145666

Category: Medical

Page: 560

View: 5947

A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.
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Design, Synthesis, Evaluation

Author: Stefan Bräse

Publisher: Royal Society of Chemistry

ISBN: 1782622241

Category: Science

Page: 468

View: 3172

One strategy to expedite the discovery of new drugs, a process that is somewhat slow and serendipitous, is the identification and use of privileged scaffolds. This book covers the history of the discovery and use of privileged scaffolds and addresses the various classes of these important molecular fragments. The first of the benzodiazepines, a class of drugs that is powerful for treating anxiety, may not have been discovered had it not been for a chance experiment on the contents of a discarded flask found during a lab clean-up. Some years later, scientists discovered that benzodiazepine derivatives were also effective in treating other diseases. This class of molecules was the first to be described as privileged in the sense that it is especially effective at altering the course of disease. Other privileged molecular structures have since been discovered, and since these compounds are so effective at interacting with numerous classes of proteins, they may be an effective starting point to look for new drugs against the supposedly “undruggable” proteins. Following introductory chapters presenting an overview, a historical perspective and the theoretical background and findings, main chapters describe the structure of privileged structures in turn and discuss major drug classes associated with them and their syntheses. This book provides comprehensive coverage of the subject through chapters contributed by expert authors from both academia and industry and will be an excellent reference source for medicinal chemists of a range of disciplines and experiences.
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Author: Iwao Ojima

Publisher: John Wiley & Sons

ISBN: 9780470744086

Category: Science

Page: 640

View: 9194

The extraordinary potential of fluorine-containing molecules in medicinal chemistry and chemical biology has been recognized by researchers outside of the traditional fluorine chemistry field, and thus a new wave of fluorine chemistry is rapidly expanding its biomedical frontiers. With several of the best selling drugs in the world crucially containing fluorine atoms, the incorporation of fluorine to drug leads has become an essential practice in biomedical research, especially for drug design and discovery as well as development. Focusing on the unique and significant roles that fluorine plays in medicinal chemistry and chemical biology, this book reviews recent advances and future prospects in this rapidly developing field. Topics covered include: Discovery and development of fluorine containing drugs and drug candidates. New and efficient synthetic methods for medicinal chemistry and the optimisation of fluorine-containing drug candidates. Structural and chemical biology of fluorinated amino acids and peptides. Fluorine labels as probes in metabolic study, protein engineering and clinical diagnosis. Applications of 19F NMR spectroscopy in biomedical research. An appendix presents an invaluable index of all fluorine-containing drugs that have been approved by the US Food and Drug Administration, including information on structure and pharmaceutical action. Fluorine in Medicinal Chemistry and Chemical Biology will serve as an excellent reference source for graduate students as well as academic and industrial researchers who want to take advantage of fluorine in biomedical research.
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Innovations and Methodologies

Author: Debarshi Kar Mahapatra,Sanjay Kumar Bharti

Publisher: Taylor & Francis

ISBN: 135180023X

Category: Medical

Page: 626

View: 8779

This valuable new book, Handbook of Research on Medicinal Chemistry: Innovations and Methodologies, presents some of the latest advancements in the various fields of combinatorial chemistry, drug discovery, biochemical aspects, pharmacology of medicinal agents, current practical problems, and nutraceuticals. The editors keep the drug molecule as the central component of the volume and aim to explain the associated features essential to exhibiting pharmacological activity. With a unique combination of chapters in biology, clinical aspects, biochemistry, synthetic chemistry, medicine and technology, the volume provides broad exposure to the essential aspect of pharmaceuticals. The volume many important aspects of medicinal chemistry, including techniques in drug discovery pharmacological aspects of natural products chemical mediators: druggable targets advances in medicinal chemistry The field of medicinal chemistry is growing at an unprecedented pace, and this volume takes an interdisciplinary approach, covering a range of new research and new practices in the field. The volume takes into account the latest therapeutic guidelines put forward by the World Health Organization and the U.S Food and Drug Administration.. Topics include: drug design drug discovery natural products and supplements and nutraceuticals pharmaceutical approaches to sexual dysfunction drug resistance parasites new natural compounds and identification of new targets stereochemistry aspects in medicinal chemistry common drug interactions in daily practices Handbook of Research on Medicinal Chemistry: Innovations and Methodologies will be a valuable addition to the bookshelves of pharmaceutical scientists and faculty as well as for industry professionals.
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Author: Richard B. Silverman,Mark W. Holladay

Publisher: Academic Press

ISBN: 0123820316

Category: Medical

Page: 536

View: 5905

The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. Updates to all chapters, including new examples and references Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry Chapter 3 (Receptors): Drug-receptor interactions, cation-π and halogen bonding; atropisomers; case history of the insomnia drug suvorexant Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates
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Technology in Transition

Author: Raymond G Hill

Publisher: Elsevier Health Sciences

ISBN: 0702053163

Category: Medical

Page: 368

View: 5621

The modern pharmacopeia has enormous power to alleviate disease, and owes its existence almost entirely to the work of the pharmaceutical industry. This book provides an introduction to the way the industry goes about the discovery and development of new drugs. The first part gives a brief historical account from its origins in the mediaeval apothecaries’ trade, and discusses the changing understanding of what we mean by disease, and what therapy aims to achieve, as well as summarising case histories of the discovery and development of some important drugs. The second part focuses on the science and technology involved in the discovery process: the stages by which a promising new chemical entity is identified, from the starting point of a medical need and an idea for addressing it. A chapter on biopharmaceuticals, whose discovery and development tend to follow routes somewhat different from synthetic compounds, is included here, as well as accounts of patent issues that arise in the discovery phase, and a chapter on research management in this environment. The third section of the book deals with drug development: the work that has to be undertaken to turn the drug candidate that emerges from the discovery process into a product on the market. The definitive introduction to how a pharmaceutical company goes about its business of discovering and developing drugs. The second edition has a new editor: Professor Raymond Hill ● non-executive director of Addex Pharmaceuticals, Covagen and of Orexo AB ● Visiting Industrial Professor of Pharmacology in the University of Bristol ● Visiting Professor in the School of Medical and Health Sciences at the University of Surrey ● Visiting Professor in Physiology and Pharmacology at the University of Strathclyde ● President and Chair of the Council of the British Pharmacological Society ● member of the Nuffield Council on Bioethics and the Advisory Council on Misuse of Drugs. New to this edition: Completely rewritten chapter on The Role of Medicinal Chemistry in the Drug Discovery Process. New topic - DMPK Optimization Strategy in drug discovery. New chapter on Scaffolds: Small globular proteins as antibody substitutes. Totally updated chapters on Intellectual Property and Marketing 50 new illustrations in full colour Features Accessible, general guide to pharmaceutical research and development. Examines the interfaces between cost and social benefit, quality control and mass production, regulatory bodies, patent management, and all interdisciplinary intersections essential to effective drug development. Written by a strong team of scientists with long experience in the pharmaceutical industry. Solid overview of all the steps from lab bench to market in an easy-to-understand way which will be accessible to non-specialists. From customer reviews of the previous edition: ‘... it will have everything you need to know on this module. Deeply referenced and, thus, deeply reliable. Highly Commended in the medicine category of the BMA 2006 medical book competition Winner of the Royal Society of Medicine Library Prize for Medical Book of the Year
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A Medicinal Chemistry Perspective

Author: Hugo Kubinyi,Gerhard Müller

Publisher: John Wiley & Sons

ISBN: 3527604022

Category: Science

Page: 487

View: 4024

Chemogenomics brings together the most powerful concepts in modern chemistry and biology, linking combinatorial chemistry with genomics and proteomics. This first reference devoted to the topic covers all stages of the early drug discovery process, from target selection to compound library and lead design. With the combined expertise of 20 research groups from academia and leading pharmaceutical companies, this is a must-have for every drug developer and medicinal chemist applying the powerful methods of chemogenomics to speed up the drug discovery process.
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Author: N.A

Publisher: Newnes

ISBN: 0080994091

Category: Science

Page: 550

View: 3110

Progress in Heterocyclic Chemistry is an annual review series commissioned by the International Society of Heterocyclic Chemistry (ISHC). Volumes in the series contain both highlights of the previous year’s literature on heterocyclic chemistry and articles on new, developing topics of particular interest to heterocyclic chemists. The highlight chapters in Volume 25 are all written by leading researchers in their field, and these chapters constitute a systematic survey of the important original material reported in the literature of heterocyclic chemistry in 2012. As with previous volumes in the series, Volume 25 will enable academic and industrial chemists and advanced students to keep abreast of developments in heterocyclic chemistry in a convenient way. Recognized as the premiere review of heterocyclic chemistry Contributions from leading researchers in the field Systematic survey of the important 2012 heterocyclic chemistry literature
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Concepts, Strategies, and Applications

Author: Patrick H. Toy,Yulin Lam

Publisher: John Wiley & Sons

ISBN: 1118141636

Category: Science

Page: 560

View: 5928

Presents both the fundamental concepts and the most recent applications in solid-phase organic synthesis With its emphasis on basic concepts, Solid-Phase Organic Synthesis guides readers through all the steps needed to design and perform successful solid-phase organic syntheses. The authors focus on the fundamentals of heterogeneous supports in the synthesis of organic molecules, explaining the use of a solid material to facilitate organic synthesis. This comprehensive text not only presents the fundamentals, but also reviews the most recent research findings and applications, offering readers everything needed to conduct their own state-of-the-art science experiments. Featuring chapters written by leading researchers in the field, Solid-Phase Organic Synthesis is divided into two parts: Part One, Concepts and Strategies, discusses the linker groups used to attach the synthesis substrate to the solid support, colorimetric tests to identify the presence of functional groups, combinatorial synthesis, and diversity-oriented synthesis. Readers will discover how solid-phase synthesis is currently used to facilitate the discovery of new molecular functionality. The final chapter discusses how using a support can change or increase reaction selectivity. Part Two, Applications, presents examples of the solid-phase synthesis of various classes of organic molecules. Chapters explore general asymmetric synthesis on a support, strategies for heterocyclic synthesis, and synthesis of radioactive organic molecules, dyes, dendrimers, and oligosaccharides. Each chapter ends with a set of conclusions that underscore the key concepts and methods. References in each chapter enable readers to investigate any topic in greater depth. With its presentation of basic concepts as well as recent findings and applications, Solid-Phase Organic Synthesis is the ideal starting point for students and researchers in organic, medicinal, and combinatorial chemistry who want to take full advantage of current solid-phase synthesis techniques.
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Author: Tommy Liljefors,Povl Krogsgaard-Larsen,Ulf Madsen

Publisher: CRC Press

ISBN: 9780415282888

Category: Medical

Page: 592

View: 3287

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.
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Ligand-protein Interactions

Author: Robert M. Stroud,Janet Finer-Moore

Publisher: Royal Society of Chemistry

ISBN: 0854043659

Category: Medical

Page: 382

View: 3555

This insightful book represents the experience and understanding of the global experts in the field and spotlights both the structural and medicinal chemistry aspects of drug design. The need to 'encode' the physiological factors of pharmacology, a key area, is explored.
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Author: Jieping Zhu,Qian Wang,Meixiang Wang

Publisher: John Wiley & Sons

ISBN: 3527332375

Category: Science

Page: 512

View: 3076

Comprehensive and up–to–date, this book focuses on the latest advances in the field, such as newly developed techniques, more environmentally benign processes, broadened scopes, and completely novel MCRs. In addition to carbene–promoted MCRs and frequently applied metal–catalyzed MCRs, it also covers recently developed catalytic enantioselective variants as well as MCR in drug discovery and for the synthesis of heterocyclic molecules and macrocycles. Edited by the leading experts and with a list of authors reading like a "who′s who" in multicomponent reaction chemistry, this is definitely a must–have for every synthetic organic chemist as well as medicinal chemists working in academia and pharmaceutical companies.
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Author: Camille Georges Wermuth

Publisher: Elsevier

ISBN: 0080497772

Category: Science

Page: 736

View: 7755

The Practice of Medicinal Chemistry, 2E, is a single-volume source on the practical aspects of medicinal chemistry. The successful first edition was nicknamed "The Bible" by medicinal chemists, and the second edition has been updated, expanded and refocused to reflect developments over the last decade. Emphasis is put on how medicinal chemists conduct their search for and design of new drug entities. In contrast to competing books, it focuses on the chemistry rather than pharmacological concepts or descriptions of the various therapeutic classes of drugs. Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists who must acquire a strong knowledge of medicinal chemistry as they enter the industry. This book aims to be their practical handbook - a complete guide to the drug discovery process. * The only book available dealing with the practical aspects of medicinal chemistry * Serves as a complete guide to the drug discovery process, from conception of the molecules to drug production * Updated chapters devoted to the discovery of new lead compounds, including combinatorial chemistry
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Author: Alfred Burger

Publisher: Wiley-Interscience

ISBN: N.A

Category: Medical

Page: 1106

View: 9396

Offers access via basic and advanced search engines to broad coverage of the field of medicinal chemistry and drug discovery for medicinal chemists, biologists, pharmacologists and molecular biologists.
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Author: John Bodenhan Taylor,D. J. Triggle

Publisher: Elsevier Science

ISBN: 9780080445144

Category: Medical

Page: 881

View: 3832

This e-book comprises 8 volumes, with all chapter sections available as PDF or HTML, and includes bibliographical references and index.
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Die Entstehung der Arten

Author: Paul Wrede,Saskia Wrede

Publisher: John Wiley & Sons

ISBN: 352766873X

Category: Science

Page: 599

View: 4727

Das grundlegende Werk von Darwin On the Origin of Species liegt hier in der originalen Übersetzung durch Julius Victor Carus vor, erweitert durch zahlreiche Erläuterungen, aussagekräftige Abbildungen sowie wichtige historische Bezüge. Die Entstehung der Arten von Darwin ist für die heutige Leserschaft häufig schwierig zu verstehen. Eine hilfreiche Unterstützung erfolgt durch die farbliche Hervorhebung entscheidender Textstellen und viele fachliche Erklärungen. Darwins Analysen und Bewertungen aus den Gebieten der Botanik, Zoologie, Verhaltenslehre, Paläontologie und Entwicklungsbiologie werden in acht Beiträgen namhafter Fachwissenschaftler im Licht der gegenwärtigen Forschung beleuchtet und so wird erst die ungeheure Bedeutung und Weitsicht seines Werkes offensichtlich. Endlich liegen jetzt die Übersetzungen der beiden ebenso bahnbrechenden Aufsätze von Alfred Russel Wallace vor: der Sarawak- und Ternate-Essay. Wallace war neben Darwin der bedeutendste Evolutionsforscher seiner Zeit. Seine Arbeiten zur Evolutionsbiologie, die im Angelsächsischen hoch geschätzt sind, können als durchaus gleichrangig zu Darwins berühmtester Schrift angesehen werden. Ulrich Kutschera eröffnet das Buch mit einem Geleitwort und Reinhold Leinfelder schließt es mit einem Ausblick zur Bedeutung der Evolutionstheorie für die Zukunft des Menschen ab. Das Buch ist daher nicht nur eine unverzichtbare Lernhilfe für Schüler und Studenten, die sich mit der Evolutionsbiologie beschäftigen, sondern zusätzlich auch eine spannende weiterführende Lektüre für alle Leser mit Interesse an Wissenschaftsgeschichte.
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