The Practice of Medicinal Chemistry


Author: Camille Georges Wermuth
Publisher: Elsevier
ISBN: 0080497772
Category: Science
Page: 736
View: 3109
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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

The Practice of Medicinal Chemistry


Author: Camille Georges Wermuth,David Aldous,Pierre Raboisson,Didier Rognan
Publisher: Elsevier
ISBN: 012417213X
Category: Science
Page: 902
View: 6356
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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

The Practice of Medicinal Chemistry


Author: C. G. Wermuth
Publisher: Elsevier
ISBN: 0127444815
Category: Medical
Page: 768
View: 2749
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Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists with little or no background in medicinal chemistry. These chemists must acquire a good knowledge of medicinal chemistry during their first years in the pharmaceutical/drug discovery industry. This book aims to be their practical handbook - a complete guide to the drug discovery process. The book reviews practical aspects of Medicinal Chemistry, emphasising the daily problems met by the medicinal chemist when dealing with lead discovery/identification methodologies, with structure-activity relationship studies aimed to scale up potency and target selectivity, and when optimising pharmacokinetic and pharmaceutical properties by means of ultimate chemical modifications. This is the second edition of The Practice of Medicinal Chemistry, the first edition being published in February 1996. The new edition is thoroughly revised, with around 30% new material, and refocussed to reflect the recent developments in genomics, proteomics, high throughput screening of compounds and drug solubilisation. An effort has been made to remove the overlap that exists in the previous edition and four new chapters have been introduced. * Written by experts in the field * The first edition of The Practice of Medicinal Chemistry, published in 1996, was nicknamed 'The Bible' by medicinal chemists. * The only available book dealing with the practical aspects of medicinal chemistry, from conception of the molecules through to the production of drugs * An essential practical handbook for the medicinal chemist, working in the pharmaceutical industry, with little or no background in medicinal chemistry-a complete guide to the drug discovery process.

The Practice of Medicinal Chemistry


Author: Camille Georges Wermuth
Publisher: Academic Press
ISBN: 9780080568775
Category: Science
Page: 982
View: 2941
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The Practice of Medicinal Chemistry fills a gap in the list of available medicinal chemistry literature. It is a single-volume source on the practical aspects of medicinal chemistry. Considered ""the Bible"" by medicinal chemists, the book emphasizes the methods that chemists use to conduct their research and design new drug entities. It serves as a practical handbook about the drug discovery process, from conception of the molecules to drug production. The first part of the book covers the background of the subject matter, which includes the definition and history of medicinal chemistry, the measurement of biological activities, and the main phases of drug activity. The second part of the book presents the road to discovering a new lead compound and creating a working hypothesis. The main parts of the book discuss the optimization of the lead compound in terms of potency, selectivity, and safety. The Practice of Medicinal Chemistry can be considered a ""first-read"" or ""bedside book"" for readers who are embarking on a career in medicinal chemistry. NEW TO THIS EDITION: * Focus on chemoinformatics and drug discovery * Enhanced pedagogical features * New chapters including: - Drug absorption and transport - Multi-target drugs * Updates on hot new areas: NEW! Drug discovery and the latest techniques NEW! How potential drugs can move through the drug discovery/ development phases more quickly NEW! Chemoinformatics

The Handbook of Medicinal Chemistry

Principles and Practice
Author: Andrew Davis,Simon. E. Ward
Publisher: Royal Society of Chemistry
ISBN: 1849736251
Category: Science
Page: 753
View: 1571
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Developed to provide a comprehensive guide, the Handbook of Medicinal Chemistry has been revised and brought up to date to cover the past, present and future of the entire drug development process.

An Introduction to Medicinal Chemistry


Author: Graham Patrick
Publisher: Oxford University Press
ISBN: 0198749694
Category: Pharmaceutical chemistry
Page: 832
View: 8851
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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

Principles and Practice
Author: Frank D. King,Royal Society of Chemistry (Great Britain)
Publisher: N.A
ISBN: 9780854046317
Category: Medical
Page: 448
View: 7652
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This book introduces the principles and practices of modern medicinal chemistry and covers all aspects of drug discovery from the initial lead to final development. It teaches how to convert a lead compound into a potential drug and provides recent case histories as examples of successes. Medicinal Chemistry is unique in dealing with the subject in such a practical way and is the only book currently available to bring together all areas of the subject in one volume. This breadth of coverage is supplemented by references to specialist monographs and reviews, where the reader can find more detail on specific topics of interest if required. Medicinal Chemistry is essential reading for students studying medicinal chemistry, as it provides a grounding in all the required disciplines and subjects. It will also be of great interest to chemists, biochemists and pharmacologists either already working in or contemplating a career in the pharmaceutical and allied industries.

Foye's Principles of Medicinal Chemistry


Author: Thomas L. Lemke,David A. Williams
Publisher: Lippincott Williams & Wilkins
ISBN: 1609133455
Category: Medical
Page: 1520
View: 9283
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Acclaimed by students and instructors alike, Foye's Principles of Medicinal Chemistry is now in its Seventh Edition, featuring updated chapters plus new material that meets the needs of today's medicinal chemistry courses. This latest edition offers an unparalleled presentation of drug discovery and pharmacodynamic agents, integrating principles of medicinal chemistry with pharmacology, pharmacokinetics, and clinical pharmacy. All the chapters have been written by an international team of respected researchers and academicians. Careful editing ensures thoroughness, a consistent style and format, and easy navigation throughout the text.

The Organic Chemistry of Drug Design and Drug Action


Author: Richard B. Silverman,Mark W. Holladay
Publisher: Academic Press
ISBN: 0123820316
Category: Medical
Page: 536
View: 8718
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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

Molecules and Medicine


Author: E. J. Corey,Barbara Czakó,L?szl? K?rti
Publisher: John Wiley & Sons
ISBN: 1118361733
Category: Science
Page: 272
View: 5892
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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.

Medicinal Chemistry

A Molecular and Biochemical Approach
Author: Thomas Nogrady,Donald F. Weaver
Publisher: Oxford University Press
ISBN: 9780198026457
Category: Medical
Page: 672
View: 1989
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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.

Basic Concepts in Medicinal Chemistry


Author: Marc W. Harrold,Robin M. Zavod
Publisher: N.A
ISBN: 9781585286010
Category:
Page: 568
View: 2040
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Scaffold Hopping in Medicinal Chemistry


Author: Nathan Brown
Publisher: Wiley-VCH
ISBN: 9783527333646
Category: Medical
Page: 328
View: 7744
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This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here.

Medicinal Natural Products

A Biosynthetic Approach
Author: Paul M. Dewick
Publisher: John Wiley & Sons
ISBN: 1119964571
Category: Science
Page: 550
View: 8859
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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.

Bioisosteres in Medicinal Chemistry


Author: Nathan Brown
Publisher: John Wiley & Sons
ISBN: 3527654321
Category: Medical
Page: 256
View: 6778
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Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.

Fluorine in Medicinal Chemistry and Chemical Biology


Author: Iwao Ojima
Publisher: John Wiley & Sons
ISBN: 9780470744086
Category: Science
Page: 640
View: 1893
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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.

Heterocyclic Chemistry in Drug Discovery


Author: Jie Jack Li
Publisher: John Wiley & Sons
ISBN: 1118354435
Category: Science
Page: 720
View: 7176
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Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.

Evaluation of Enzyme Inhibitors in Drug Discovery

A Guide for Medicinal Chemists and Pharmacologists
Author: Robert A. Copeland
Publisher: John Wiley & Sons
ISBN: 111854028X
Category: Science
Page: 572
View: 5233
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Offers essential guidance for discovering and optimizing novel drug therapies Using detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the tools needed to apply the science of enzymology and biochemistry to the discovery, optimization, and preclinical development of drugs that work by inhibiting specific enzyme targets. Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid. This Second Edition brings the book thoroughly up to date with the latest research findings and practices. Updates explore additional forms of enzyme inhibition and special treatments for enzymes that act on macromolecular substrates. Readers will also find new discussions detailing the development and application of the concept of drug-target residence time. Evaluation of Enzyme Inhibitors in Drug Discovery begins by explaining why enzymes are such important drug targets and then examines enzyme reaction mechanisms. The book covers: Reversible modes of inhibitor interactions with enzymes Assay considerations for compound library screening Lead optimization and structure-activity relationships for reversible inhibitors Slow binding and tight binding inhibitors Drug-target residence time Irreversible enzyme inactivators The book ends with a new chapter exploring the application of quantitative biochemical principles to the pharmacologic evaluation of drug candidates during lead optimization and preclinical development. The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery continues to offer a treatment of enzymology applied to drug discovery that is quantitative and mathematically rigorous. At the same time, the clear and simple presentations demystify the complex science of enzymology, making the book accessible to many fields— from pharmacology to medicinal chemistry to biophysics to clinical medicine.

Pharmaceutical Chemistry


Author: Jill Barber,Chris Rostron
Publisher: Oxford University Press
ISBN: 0199655308
Category: Medical
Page: 368
View: 9274
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Taking medication is a common occurrence for many people, whether it is to soothe an aching head, regulate blood sugars, or treat life-threatening conditions such as HIV or cancer. Examining how drugs are manufactured, formulated, and the way that they work in our bodies, Pharmaceutical Chemistry provides a wide-ranging overview of organic chemistry as it is applied to the study and practice of pharmacy. FEATURES * Supports an integrated pharmacy education * Focuses on the fundamental ideas that first-year students need to fully grasp before progressing in their studies * Demonstrates the connections between scientific concepts and principles and how they are applied to pharmacy * Written and edited by experts who have a wealth of teaching experience COMPANION WEBSITE For registered adopters of the book: - Figures from the book, available to download For students: - Self-assessment questions for each chapter - Related additional resources ABOUT THE SERIES The Integrated Foundations of Pharmacy series supports those who are at the beginning of their journey to become a pharmacist. Students will begin to understand how a drug molecule is made; the process that turns it into a medicine; the role the pharmacist has when dispensing that medicine; and what happens in the body when it is taken. Most importantly, the series shows how each of these aspects are integrated, reflecting the most up-to-date teaching practices.

Essentials of Organic Chemistry

For Students of Pharmacy, Medicinal Chemistry and Biological Chemistry
Author: Paul M. Dewick
Publisher: John Wiley & Sons
ISBN: 1118681967
Category: Science
Page: 704
View: 5558
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Essentials of Organic Chemistry is an accessible introduction to the subject for students of Pharmacy, Medicinal Chemistry and Biological Chemistry. Designed to provide a thorough grounding in fundamental chemical principles, the book focuses on key elements of organic chemistry and carefully chosen material is illustrated with the extensive use of pharmaceutical and biochemical examples. In order to establish links and similarities the book places prominence on principles and deductive reasoning with cross-referencing. This informal text also places the main emphasis on understanding and predicting reactivity rather than synthetic methodology as well as utilising a mechanism based layout and featuring annotated schemes to reduce the need for textual explanations. * tailored specifically to the needs of students of Pharmacy Medical Chemistry and Biological Chemistry * numerous pharmaceutical and biochemical examples * mechanism based layout * focus on principles and deductive reasoning This will be an invaluable reference for students of Pharmacy Medicinal and Biological Chemistry.