Lead Optimization for Medicinal Chemists

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Publisher : John Wiley & Sons
ISBN 13 : 3527645659
Total Pages : 627 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Lead Optimization for Medicinal Chemists by : Florencio Zaragoza Dörwald

Download or read book Lead Optimization for Medicinal Chemists written by Florencio Zaragoza Dörwald and published by John Wiley & Sons. This book was released on 2013-02-04 with total page 627 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small structural modifications can significantly affect the pharmacokinetic properties of drug candidates. This book, written by a medicinal chemist for medicinal chemists, is a comprehensive guide to the pharmacokinetic impact of functional groups, the pharmacokinetic optimization of drug leads, and an exhaustive collection of pharmacokinetic data, arranged according to the structure of the drug, not its target or indication. The historical origins of most drug classes and general aspects of modern drug discovery and development are also discussed. The index contains all the drug names and synonyms to facilitate the location of any drug or functional group in the book. This compact working guide provides a wealth of information on the ways small structural modifications affect the pharmacokinetic properties of organic compounds, and offers plentiful, fact-based inspiration for the development of new drugs. This book is mainly aimed at medicinal chemists, but may also be of interest to graduate students in chemical or pharmaceutical sciences, preparing themselves for a job in the pharmaceutical industry, and to healthcare professionals in need of pharmacokinetic data.

Accounts in Drug Discovery

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Publisher : Royal Society of Chemistry
ISBN 13 : 1849731268
Total Pages : 397 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis Accounts in Drug Discovery by : Joel Barrish

Download or read book Accounts in Drug Discovery written by Joel Barrish and published by Royal Society of Chemistry. This book was released on 2011 with total page 397 pages. Available in PDF, EPUB and Kindle. Book excerpt: Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high-throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first-generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof-of-concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses," i.e. exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, the Editors believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists.

Lead Generation

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Publisher : John Wiley & Sons
ISBN 13 : 3527677070
Total Pages : 824 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Lead Generation by : Jörg Holenz

Download or read book Lead Generation written by Jörg Holenz and published by John Wiley & Sons. This book was released on 2016-03-16 with total page 824 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation.

Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 111953030X
Total Pages : 6057 pages
Book Rating : 4.1/5 (195 download)

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Book Synopsis Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set by :

Download or read book Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set written by and published by John Wiley & Sons. This book was released on 2021-04-20 with total page 6057 pages. Available in PDF, EPUB and Kindle. Book excerpt: Burger’s Medicinal Chemistry, Drug Discovery and Development Explore the freshly updated flagship reference for medicinal chemists and pharmaceutical professionals The newly revised eighth edition of the eight-volume Burger’s Medicinal Chemistry, Drug Discovery and Development is the latest installment in this celebrated series covering the entirety of the drug development and discovery process. With the addition of expert editors in each subject area, this eight-volume set adds 35 chapters to the extensive existing chapters. New additions include analyses of opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures. Along with the incorporation of practical material on drug hunting, the set features sections on drug discovery, drug development, cardiovascular diseases, metabolic diseases, immunology, cancer, anti-Infectives, and CNS disorders. The text continues the legacy of previous volumes in the series by providing recognized, renowned, authoritative, and comprehensive information in the area of drug discovery and development while adding cutting-edge new material on issues like the use of artificial intelligence in medicinal chemistry. Included: Volume 1: Methods in Drug Discovery, edited by Kent D. Stewart Volume 2: Discovering Lead Molecules, edited by Kent D. Stewart Volume 3: Drug Development, edited by Ramnarayan S. Randad and Michael Myers Volume 4: Cardiovascular, Endocrine, and Metabolic Diseases, edited by Scott D. Edmondson Volume 5: Pulmonary, Bone, Immunology, Vitamins, and Autocoid Therapeutic Agents, edited by Bryan H. Norman Volume 6: Cancer, edited by Barry Gold and Donna M. Huryn Volume 7: Anti-Infectives, edited by Roland E. Dolle Volume 8: CNS Disorders, edited by Richard A. Glennon Perfect for research departments in the pharmaceutical and biotechnology industries, Burger’s Medicinal Chemistry, Drug Discovery and Development can be used by graduate students seeking a one-stop reference for drug development and discovery and deserves its place in the libraries of biomedical research institutes, medical, pharmaceutical, and veterinary schools.

The Practice of Medicinal Chemistry

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Publisher :
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (975 download)

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Book Synopsis The Practice of Medicinal Chemistry by : Camille Georges Wermuth

Download or read book The Practice of Medicinal Chemistry written by Camille Georges Wermuth and published by . This book was released on 2016 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Evaluation of Enzyme Inhibitors in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 0471723266
Total Pages : 295 pages
Book Rating : 4.4/5 (717 download)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland and published by John Wiley & Sons. This book was released on 2005-04-01 with total page 295 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." -Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: * What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? * How are inhibitors evaluated for potency, selectivity, and mode of action? * What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? * What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.

Physicochemical and Biomimetic Properties in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 1118770323
Total Pages : 354 pages
Book Rating : 4.1/5 (187 download)

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Book Synopsis Physicochemical and Biomimetic Properties in Drug Discovery by : Klara Valko

Download or read book Physicochemical and Biomimetic Properties in Drug Discovery written by Klara Valko and published by John Wiley & Sons. This book was released on 2013-11-25 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: Demonstrating how and why to measure physicochemical and biomimetic properties in early stages of drug discovery for lead optimization, Physicochemical and Biomimetic Properties in Drug Discovery encourages readers to discover relationships between various measurements and develop a sense of interdisciplinary thinking that will add to new research in drug discovery. This practical guide includes detailed descriptions of state-of-the-art chromatographic techniques and uses real-life examples and models to help medicinal chemists and scientists and advanced graduate students apply measurement data for optimal drug discovery.

Fragment-Based Drug Discovery

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Publisher : Royal Society of Chemistry
ISBN 13 : 1782625658
Total Pages : 314 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Fragment-Based Drug Discovery by : Steven Howard

Download or read book Fragment-Based Drug Discovery written by Steven Howard and published by Royal Society of Chemistry. This book was released on 2015-06-17 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.

Medicinal Chemistry

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Publisher : Garland Science
ISBN 13 : 1351586203
Total Pages : 944 pages
Book Rating : 4.3/5 (515 download)

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Book Synopsis Medicinal Chemistry by : Norma K Dunlap

Download or read book Medicinal Chemistry written by Norma K Dunlap and published by Garland Science. This book was released on 2018-04-17 with total page 944 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry begins with the history of the field, starting from the serendipitous use of plant preparations to current practice of design- and target-based screening methods. Written from the perspective of practicing medicinal chemists, the text covers key drug discovery activities such as pharmacokinetics and patenting, as well as the classes and structures of drug targets (receptors, enzymes, nucleic acids, and protein-protein and lipid interactions) with numerous examples of drugs acting at each type. Selected therapeutic areas include drugs to treat cancer, infectious diseases, and central nervous system disorders. Throughout the book, historical and current examples illustrate the progress to market and case studies explore the applications of concepts discussed in the text. Each chapter features a Journal Club, as well as review and application questions to enhance and test comprehension. This textbook is ideal for upper-level undergraduates and graduate students taking a one-semester survey course on medicinal chemistry and/or drug discovery, as well as scientists entering the pharmaceutical industry.

Evaluation of Enzyme Inhibitors in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 111854028X
Total Pages : 588 pages
Book Rating : 4.1/5 (185 download)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland and published by John Wiley & Sons. This book was released on 2013-01-31 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

New Synthetic Technologies in Medicinal Chemistry

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Publisher : Royal Society of Chemistry
ISBN 13 : 1849733058
Total Pages : 177 pages
Book Rating : 4.8/5 (497 download)

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Book Synopsis New Synthetic Technologies in Medicinal Chemistry by : Elizabeth Farrant

Download or read book New Synthetic Technologies in Medicinal Chemistry written by Elizabeth Farrant and published by Royal Society of Chemistry. This book was released on 2011-10-04 with total page 177 pages. Available in PDF, EPUB and Kindle. Book excerpt: The modern synthetic chemist applies all the tools available to identify the drug-like molecules with the best chances of becoming novel drugs. This book will act as a primer for graduates and postgraduates interested in a career in drug discovery. It covers both synthetic technologies currently impacting medicinal chemistry and emerging areas. The chapters focus on topics including: parallel medicinal chemistry; solid supported reagents; microwave assisted chemistry; flow synthesis, and high throughput reaction screening.

Medicinal Chemistry for Practitioners

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Publisher : John Wiley & Sons
ISBN 13 : 1119607302
Total Pages : 416 pages
Book Rating : 4.1/5 (196 download)

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Book Synopsis Medicinal Chemistry for Practitioners by : Jie Jack Li

Download or read book Medicinal Chemistry for Practitioners written by Jie Jack Li and published by John Wiley & Sons. This book was released on 2020-06-29 with total page 416 pages. Available in PDF, EPUB and Kindle. Book excerpt: Presenting both a panoramic introduction to the essential disciplines of drug discovery for novice medicinal chemists as well as a useful reference for veteran drug hunters, this book summarizes the state-of-the-art of medicinal chemistry. It covers key drug targets including enzymes, receptors, and ion channels, and hit and lead discovery. The book hen surveys a drug's pharmacokinetics and toxicity, with a solid chapter covering fundamental bioisosteres as a guide to structure-activity relationship investigations.

The Handbook of Medicinal Chemistry

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Publisher : Royal Society of Chemistry
ISBN 13 : 1782621830
Total Pages : 789 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis The Handbook of Medicinal Chemistry by : Andrew Davis

Download or read book The Handbook of Medicinal Chemistry written by Andrew Davis and published by Royal Society of Chemistry. This book was released on 2015-07-07 with total page 789 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug discovery is a constantly developing and expanding area of research. Developed to provide a comprehensive guide, the Handbook of Medicinal Chemistry covers the past, present and future of the entire drug development process. Highlighting the recent successes and failures in drug discovery, the book helps readers to understand the factors governing modern drug discovery from the initial concept through to a marketed medicine. With chapters covering a wide range of topics from drug discovery processes and optimization, development of synthetic routes, pharmaceutical properties and computational biology, the handbook aims to enable medicinal chemists to apply their academic understanding to every aspect of drug discovery. Each chapter includes expert advice to not only provide a rigorous understanding of the principles being discussed, but to provide useful hints and tips gained from within the pharmaceutical industry. This expertise, combined with project case studies, highlighting and discussing all areas of successful projects, make this an essential handbook for all those involved in pharmaceutical development.

The Organic Chemistry of Drug Design and Drug Action

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Publisher : Elsevier
ISBN 13 : 0080513379
Total Pages : 650 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis The Organic Chemistry of Drug Design and Drug Action by : Richard B. Silverman

Download or read book The Organic Chemistry of Drug Design and Drug Action written by Richard B. Silverman and published by Elsevier. This book was released on 2012-12-02 with total page 650 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Drug-like Properties: Concepts, Structure Design and Methods

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Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Basic Principles of Drug Discovery and Development

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Publisher : Academic Press
ISBN 13 : 0128172150
Total Pages : 738 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Basic Principles of Drug Discovery and Development by : Benjamin E. Blass

Download or read book Basic Principles of Drug Discovery and Development written by Benjamin E. Blass and published by Academic Press. This book was released on 2021-03-30 with total page 738 pages. Available in PDF, EPUB and Kindle. Book excerpt: Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, which requires a multidisciplinary team approach with input from medicinal chemists, biologists, pharmacologists, drug metabolism experts, toxicologists, clinicians, and a host of experts from numerous additional fields. Enabling technologies such as high throughput screening, structure-based drug design, molecular modeling, pharmaceutical profiling, and translational medicine are critical to the successful development of marketable therapeutics. Given the wide range of disciplines and techniques that are required for cutting edge drug discovery and development, a scientist must master their own fields as well as have a fundamental understanding of their collaborator's fields. This book bridges the knowledge gaps that invariably lead to communication issues in a new scientist's early career, providing a fundamental understanding of the various techniques and disciplines required for the multifaceted endeavor of drug research and development. It provides students, new industrial scientists, and academics with a basic understanding of the drug discovery and development process. The fully updated text provides an excellent overview of the process and includes chapters on important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles of in vivo pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. - Provides a clear explanation of how the pharmaceutical industry works, as well as the complete drug discovery and development process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual property - Includes a new chapter on the discovery and development of biologics (antibodies proteins, antibody/receptor complexes, antibody drug conjugates), a growing and important area of the pharmaceutical industry landscape - Features a new section on formulations, including a discussion of IV formulations suitable for human clinical trials, as well as the application of nanotechnology and the use of transdermal patch technology for drug delivery - Updated chapter with new case studies includes additional modern examples of drug discovery through high through-put screening, fragment-based drug design, and computational chemistry

Thermodynamics and Kinetics of Drug Binding

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 352733582X
Total Pages : 360 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Thermodynamics and Kinetics of Drug Binding by : György Keserü

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.