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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



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.



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.



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



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 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



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



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.



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



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



Principles of Asymmetric Synthesis

Principles of Asymmetric Synthesis Author Robert E. Gawley
ISBN-10 9780080448602
Release 2012
Pages 555
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The world is chiral. Most of the molecules in it are chiral, and asymmetric synthesis is an important means by which enantiopure chiral molecules may be obtained for study and sale. Using examples from the literature of asymmetric synthesis (more than 1300 references), the aim of this book is to present a detailed analysis of the factors that govern stereoselectivity in organic reactions. It is important to note that the references were each individually checked by the authors to verify relevance to the topics under discussion. The study of stereoselectivity has evolved from issues of diastereoselectivity, through auxiliary-based methods for the synthesis of enantiomerically pure compounds (diastereoselectivity followed by separation and auxiliary cleavage), to asymmetric catalysis. In the latter instance, enantiomers (not diastereomers) are the products, and highly selective reactions and modern purification techniques allow preparation - in a single step - of chiral substances in 99% ee for many reaction types. After an explanation of the basic physical-organic principles of stereoselectivity, the authors provide a detailed, annotated glossary of stereochemical terms. A chapter on "Analytical Methods" provides a critical overview of the most common methods for analysis of stereoisomers. The authors then follow the 'tried-and-true' format of grouping the material by reaction type. Thus, there are four chapters on carbon-carbon bond forming reactions (enolate alkylations, organometal additions to carbonyls, aldol and Michael reactions, and cycloadditions and rearrangements), one chapter on reductions and hydroborations (carbon-hydrogen bond forming reactions), and one on oxidations (carbon-oxygen and carbon-nitrogen bond forming reactions). Leading references are provided to natural product synthesis that have been accomplished using a given reaction as a key step. In addition to tables of examples that show high selectivity, a transition state analysis is presented to explain - to the current level of understanding - the stereoselectivity of each reaction. In one case (Cram's rule) the evolution of the current theory is detailed from its first tentative (1952) postulate to the current Felkin-Anh-Heathcock formalism. For other reactions, only the currently accepted rationale is presented. Examination of these rationales also exposes the weaknesses of current theories, in that they cannot always explain the experimental observations. These shortcomings provide a challenge for future mechanistic investigations. Authoritative glossary to aid understanding of stereochemical terminology Explanations of the key factors influencing stereoselectivity with numerous examples, organized by reaction type A handy reference guide to the literature of asymmetric synthesis for practitioners in the field



Medicinal Natural Products

Medicinal Natural Products Author Paul M. Dewick
ISBN-10 9781119964575
Release 2011-09-20
Pages 550
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Medicinal Natural Products: A Biosynthetic Approach, Third Edition, provides a comprehensive and balanced introduction to natural products from a biosynthetic perspective, focussing on the metabolic sequences leading to various classes of natural products. The book builds upon fundamental chemical principles and guides the reader through a wealth of diverse natural metabolites with particular emphasis on those used in medicine. There have been rapid advances in biosynthetic understanding over the past decade through enzymology, gene isolation and genetic engineering. Medicinal Natural Products has been extended and fully updated in this new edition to reflect and explain these developments and other advances in the field. It retains the user-friendly style and highly acclaimed features of previous editions: a comprehensive treatment of plant, microbial, and animal natural products in one volume extensive use of chemical schemes with annotated mechanistic explanations cross-referencing to emphasize links and similarities boxed topics giving further details of medicinal materials, covering sources, production methods, use as drugs, semi-synthetic derivatives and synthetic analogues, and modes of action Medicinal Natural Products: A Biosynthetic Approach, Third Edition, is an invaluable textbook for students of pharmacy, pharmacognosy, medicinal chemistry, biochemistry and natural products chemistry.



Pharmacokinetics and Metabolism in Drug Design

Pharmacokinetics and Metabolism in Drug Design Author Dennis A. Smith
ISBN-10 9783527645299
Release 2012-09-13
Pages 268
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In this new edition of a bestseller, all the contents have been brought upto-date by addressing current standards and best practices in the assessment and prediction of ADMET properties. Although the previous chapter layout has been retained, substantial revisions have been made, with new topics such as pro-drugs, active metabolites and transporters covered in detail in a manner useful to the Drug Discovery scientist. The authors discuss the parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects. Uniquely comprehensive, the book relates physicochemistry and chemical structure to pharmacokinetic properties and ultimately drug efficacy and safety.



Review of Organic Functional Groups

Review of Organic Functional Groups Author Thomas L. Lemke
ISBN-10 0781743818
Release 2003
Pages 156
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Designed to be used as a self-paced review, this text outlines the functional groups common to organic chemistry, reviewing the general topics of nomenclature, physical and chemical properties, and metabolism. The text provides background material for the formal pharmacy courses in medicinal chemistry, easing the transition from general organic chemistry courses required of all pre-pharmacy students. The Fourth Edition will include a workbook on CD-ROM as well as an index on general drug metabolism. Students who use this text are able to complete difficult tasks such as: drawing a chemical structure or official chemical name; predicting solubility of chemicals in liquids; predicting and showing, with chemical structures, the metabolism of organic functional groups; predicting and showing instabilities, with chemical structures.



A Pharmacology Primer

A Pharmacology Primer Author Terry Kenakin
ISBN-10 9780124076891
Release 2014-03-26
Pages 450
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A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, 4th Edition features the latest ideas and research about the application of pharmacology to the process of drug discovery to equip readers with a deeper understanding of the complex and rapid changes in this field. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for all those involved in drug discovery. This edition has been thoroughly revised to include material on data-driven drug discovery, biased signaling, structure-based drug design, drug activity screening, drug development (including pharmacokinetics and safety Pharmacology), and much more. With more color illustrations, examples, and exercises throughout, this book remains a top reference for all industry and academic scientists and students directly involved in drug discovery, or pharmacologic research. Highlights changes surrounding the strategy of drug discovery to provide you with a comprehensive reference featuring advances in the methods involved in lead optimization and more effective drug discovery Includes a new chapter on data-driven drug discovery in terms of the optimal design of pharmacological experiments to identify mechanism of action of new molecules Illustrates the application of rapid inexpensive assays to predict activity in the therapeutic setting, showing data outcomes and the limitations inherent in interpreting this data