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The Organic Chemistry of Drug Design and Drug Action

The Organic Chemistry of Drug Design and Drug Action Author Richard B. Silverman
ISBN-10 9780123820310
Release 2014-03-29
Pages 536
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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



The Organic Chemistry of Drug Design and Drug Action

The Organic Chemistry of Drug Design and Drug Action Author Richard B. Silverman
ISBN-10 9780080513379
Release 2012-12-02
Pages 617
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Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization



The Organic Chemistry of Drug Design and Drug Action

The Organic Chemistry of Drug Design and Drug Action Author Richard B. Silverman
ISBN-10 9780080571232
Release 2012-12-02
Pages 422
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This is a new approach to the teaching of medicinal chemistry. The knowledge of the physical organic chemical basis of drug design and drug action allows the reader to extrapolate to the many related classes of drugs described in standard medicinal chemistry texts. Students gain a solid foundation to base future research endeavors upon: drugs not yet developed are thus covered! n Emphasizes the use of the principles of physical organic chemistry as a basis for drug design n Discusses organic reaction mechanisms of clinically important drugs with mechanistic schemes n Uses figures and literature references extensively throughout n This text is not merely a "compilation of drugs and uses," but features selected drugs as examples of the organic chemical basis for any and all drug design applications



The Organic Chemistry of Drug Design and Drug Action Power PDF

The Organic Chemistry of Drug Design and Drug Action  Power PDF Author Richard B. Silverman
ISBN-10 9780080575384
Release 2005-02-04
Pages 1275
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This CD-ROM edition of Silverman's Organic Chemisry of Drug Design and Drug Action, Second Edition reflects the significant changes in the drug industry in recent years, using an accessible interactive approach. This CD-ROM integrates the author's own PowerPoint slides, indexed and linked to the book pages in PDF format. The three-part structure includes an all-electronic text with full-text search capabilites and nearly 800 powerpoint slides. This is a unique and powerful combination of electronic study guide and full book pages. Users can hyperlink seamlessly from the main text to key points and figures on the outline and back again. It serves as a wonderful supplement for instructors as well as a fully integrated text and study aid for students. * Three-part package includes 1) powerpoint, 2) integrated powerpoint and pdf-based text, and 3) fully searchable PDF-based text with index * Includes new full-color illustrations, structures, schemes, and figures as well as extensive chapter problems and exercises * User-friendly buttons transition from overview (study-guide) format to corresponding book page and back with the click of a mouse * Full-text search capabality an incomparable tool for researchers seeking specific references and/or unindexed phrases



An Introduction to Medicinal Chemistry

An Introduction to Medicinal Chemistry Author Graham Patrick
ISBN-10 9780198749691
Release 2017
Pages 832
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For many people, taking some form of medication is part of everyday life, whether for mild or severe illness, acute or chronic disease, to target infection or to relieve pain. However for most it remains a mystery as to what happens once the drug has been taken into the body: how do the drugs actually work? Furthermore, by what processes are new drugs discovered and brought to market?An Introduction to Medicinal Chemistry, sixthedition, provides an accessible and comprehensive account of this fascinating multidisciplinary field. Assuming little prior knowledge, the text is ideal for those studying the subject for the first time. Inaddition to covering the key principles of drug design and drug action, the text also discusses important current topics in medicinal chemistry. The subject is brought to life throughout by engaging case studies highlighting particular classes of drugs, and the stories behind their discovery and development.



Medicinal Chemistry

Medicinal Chemistry Author Thomas Nogrady
ISBN-10 9780190282967
Release 2005-08-11
Pages
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Fully updated and rewritten by a basic scientist who is also a practicing physician, the third edition of this popular textbook remains comprehensive, authoritative and readable. Taking a receptor-based, target-centered approach, it presents the concepts central to the study of drug action in a logical, mechanistic way grounded on molecular and principles. Students of pharmacy, chemistry and pharmacology, as well as researchers interested in a better understanding of drug design, will find this book an invaluable resource. Starting with an overview of basic principles, Medicinal Chemistry examines the properties of drug molecules, the characteristics of drug receptors, and the nature of drug-receptor interactions. Then it systematically examines the various families of receptors involved in human disease and drug design. The first three classes of receptors are related to endogenous molecules: neurotransmitters, hormones and immunomodulators. Next, receptors associated with cellular organelles (mitochondria, cell nucleus), endogenous macromolecules (membrane proteins, cytoplasmic enzymes) and pathogens (viruses, bacteria) are examined. Through this evaluation of receptors, all the main types of human disease and all major categories of drugs are considered. There have been many changes in the third edition, including a new chapter on the immune system. Because of their increasingly prominent role in drug discovery, molecular modeling techniques, high throughput screening, neuropharmacology and genetics/genomics are given much more attention. The chapter on hormonal therapies has been thoroughly updated and re-organized. Emerging enzyme targets in drug design (e.g. kinases, caspases) are discussed, and recent information on voltage-gated and ligand-gated ion channels has been incorporated. The sections on antihypertensive, antiviral, antibacterial, anti-inflammatory, antiarrhythmic, and anticancer drugs, as well as treatments for hyperlipidemia and peptic ulcer, have been substantially expanded. One new feature will enhance the book's appeal to all readers: clinical-molecular interface sections that facilitate understanding of the treatment of human disease at a molecular level.



Drug Discovery

Drug Discovery Author Jie Jack Li
ISBN-10 9781118354469
Release 2013-04-03
Pages 570
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Sets forth the history, state of the science, and future directions of drug discovery Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection, biological testing, drug metabolism, and computer-assisted drug design. Drug Discovery features chapters written by an international team of pharmaceutical and medicinal chemists. Contributions are based on a thorough review of the current literature as well as the authors' firsthand laboratory experience in drug discovery. The book begins with the history of drug discovery, describing groundbreaking moments in the field. Next, it covers such topics as: Target identification and validation Drug metabolism and pharmacokinetics Central nervous system drugs In vitro and in vivo assays Cardiovascular drugs Cancer drugs Each chapter features a case study, helping readers understand how science is put into practice throughout all phases of drug discovery. References at the end of each chapter serve as a gateway to groundbreaking original research studies and reviews in the field. Drug Discovery is ideal for newcomers to medicinal chemistry and drug discovery, providing a comprehensive overview of the field. Veterans in the field will also benefit from the perspectives of leading international experts in all aspects of drug discovery.



Molecules and Medicine

Molecules and Medicine Author E. J. Corey
ISBN-10 9781118361733
Release 2012-02-28
Pages 272
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Molecules and Medicine provides, for the first time ever, a completely integrated look at chemistry, biology, drug discovery, and medicine. It delves into the discovery, application, and mode of action of more than one hundred of the most significant molecules in use in modern medicine. Opening sections of the book provide a unique, clear, and concise introduction, which enables readers to understand chemical formulas.



The Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry Author Camille Georges Wermuth
ISBN-10 9780124172135
Release 2015-07-01
Pages 902
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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



Drug Like Properties

Drug Like Properties Author Li Di
ISBN-10 9780128013229
Release 2015-12-17
Pages 580
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Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property. Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization. Provides a comprehensive and valuable working handbook for scientists and students in medicinal chemistry Includes expanded coverage of pharmacokinetics fundamentals and effects Contains updates throughout, including the authors’ recent work in the importance of solubility in drug development; new and currently used property methods, with a reduction of seldom-used methods; and exploration of computational modeling methods



Medicinal Chemistry

Medicinal Chemistry Author Gareth Thomas
ISBN-10 9781119965428
Release 2011-09-20
Pages 646
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Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and multidisciplinary area of research. Building on the success of the First Edition, this edition has been completely revised and updated to include the latest developments in the field. Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles, assuming little in the way of prior knowledge. The book focuses on the chemical principles used for drug discovery and design covering physiology and biology where relevant. It opens with a broad overview of the subject with subsequent chapters examining topics in greater depth. From the reviews of the First Edition: "It contains a wealth of information in a compact form" ANGEWANDTE CHEMIE, INTERNATIONAL EDITION "Medicinal Chemistry is certainly a text I would chose to teach from for undergraduates. It fills a unique niche in the market place." PHYSICAL SCIENCES AND EDUCATIONAL REVIEWS



Essentials of Pharmaceutical Chemistry

Essentials of Pharmaceutical Chemistry Author Donald Cairns
ISBN-10 9780853699798
Release 2012-01-01
Pages 308
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An introduction to pharmaceutical chemistry for undergraduate pharmacy, chemistry and medicinal chemistry students. Essentials of Pharmaceutical Chemistry is a chemistry introduction that covers all of the core material necessary to provide an understanding of the basic chemistry of drug molecules. Now a core text on many university courses, it contains numerous worked examples and problems. The 4th edition includes new chapters on Chromatographic Methods of Analysis, and Medicinal Chemistry - The Science of Drug Design.



Organic Chemistry of Enzyme Catalyzed Reactions Revised Edition

Organic Chemistry of Enzyme Catalyzed Reactions  Revised Edition Author Richard B. Silverman
ISBN-10 9780080513362
Release 2002-03-07
Pages 800
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The Organic Chemistry of Enzyme-Catalyzed Reactions is not a book on enzymes, but rather a book on the general mechanisms involved in chemical reactions involving enzymes. An enzyme is a protein molecule in a plant or animal that causes specific reactions without itself being permanently altered or destroyed. This is a revised edition of a very successful book, which appeals to both academic and industrial markets. Illustrates the organic mechanism associated with each enzyme-catalyzed reaction Makes the connection between organic reaction mechanisms and enzyme mechanisms Compiles the latest information about molecular mechanisms of enzyme reactions Accompanied by clearly drawn structures, schemes, and figures Includes an extensive bibliography on enzyme mechanisms covering the last 30 years Explains how enzymes can accelerate the rates of chemical reactions with high specificity Provides approaches to the design of inhibitors of enzyme-catalyzed reactions Categorizes the cofactors that are appropriate for catalyzing different classes of reactions Shows how chemical enzyme models are used for mechanistic studies Describes catalytic antibody design and mechanism Includes problem sets and solutions for each chapter Written in an informal and didactic style



Drug Design and Action

Drug Design and Action Author Joaquín M. Campos Rosa
ISBN-10 9783110528480
Release 2017-08-21
Pages 186
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This two volume book is an excellent introduction to this interdisciplinary area, lying on the interface between organic chemistry, biochemistry and medicine. The authors give a comprehensive overview of the field and outline the actual challenges in pharmaceutical science and industry. Volume 1 introduces the concepts of drug design and drug metabolic processes as well as antibacterial, antiviral and anticancer agents.



Contemporary Drug Synthesis

Contemporary Drug Synthesis Author Jie Jack Li
ISBN-10 0471686735
Release 2004-12-27
Pages 240
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An integrated and insightful look at successful drug synthesis in today's drug discovery market The pharmaceutical industry is unquestionably vibrant today, with drug synthesis making a vital contribution. Whether in the early developmental stages of identifying and optimizing a lead, or the latter stages of process development and cost-effective scale-up, the ability to design elegant and economical synthetic routes is often a major factor in the eventual viability and commercial success of a drug. Contemporary Drug Synthesis examines how leading researchers and manufacturers have integrated chemistry, biology, pharmacokinetics, and a host of other disciplines in the creation and development of leading drugs. Authored by four of the pharmaceutical industry's most respected scientists, this timely volume: Focuses on the processes that resulted in high-profile drugs including Lipitor, Celebrex, Viagra, Gleevec, Nexium, Claritin, and over a dozen others Provides an in-depth introduction to each drug, followed by a detailed account of its synthesis Organizes the drugs into fourteen therapeutic areas for clarity and ease of use Process chemists provide an essential bridge between chemistry and the marketplace, creating scientifically practical drug processes while never losing sight of the commercial viability of those processes. Contemporary Drug Synthesis meets the needs of a growing community of researchers in pharmaceutical research and development, and is both a useful guide for practicing pharmaceutical scientists and an excellent text for medicinal and organic chemistry students.



The Evolution of Drug Discovery

The Evolution of Drug Discovery Author Enrique Ravina
ISBN-10 9783527326693
Release 2011-01-11
Pages 504
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Based on his profound knowledge of past and present paradigms in the development of medicines, the author takes the reader from the very beginnings of pharmacology to the multibillion-dollar business it represents today. Recounting the often spectacular successes and failures of innovative drugs as well as the people who discovered them, he brings abstract science to life in anecdotal form. The book is beautifully illustrated, containing historical photographs of drugs and their discoverers, and abounds with references to the primary literature, listing seminal publications alongside more modern reviews for readers seeking further details. For anyone with a more than superficial interest in the science of drugs: instructive and enjoyable for a broad audience of students, instructors and professionals in pharmacy, the pharmaceutical chemistry and related fields.



Fundamentals of Medicinal Chemistry

Fundamentals of Medicinal Chemistry Author Gareth Thomas
ISBN-10 9780470871690
Release 2004-04-20
Pages 302
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Provides a concise introduction to the chemistry of therapeutically active compounds, written in a readable and accessible style. The title begins by reviewing the structures and nomenclature of the more common classes of naturally occurring compounds found in biological organisms. An overview of medicinal chemistry is followed by chapters covering the discovery and design of drugs, pharmacokinetics and drug metabolism, The book concludes with a chapter on organic synthesis, followed by a brief look at drug development from the research stage through to marketing the final product. The text assumes little in the way of prior biological knowledge. relevant biology is included through biological topics, examples and the Appendices. Incorporates summary sections, examples, applications and problems Each chapter contains an additional summary section and solutions to the questions are provided at the end of the text Invaluable for undergraduates studying within the chemical, pharmaceutical and life sciences.