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Lead Optimization For Medicinal Chemists
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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.
Book Synopsis Lead-Seeking Approaches by : Matthew M. Hayward
Download or read book Lead-Seeking Approaches written by Matthew M. Hayward and published by Springer Science & Business Media. This book was released on 2010-03-12 with total page 224 pages. Available in PDF, EPUB and Kindle. Book excerpt: High quality leads provide the foundation for the discovery of successful clinical development candidates, and therefore the identi?cation of leads is an essential part of drug discovery. The process for the identi?cation of leads generally starts with the screening of a compound collection, either an HTS of a relatively large compound collection (hundreds of thousands to one million plus compounds) or a more focused screen of a smaller set of compounds that have been preselected for the target of interest. Virtual screening methods such as structure-based or pharmacophore-based searches can complement or replace one of the above approaches. Once hits are identi?ed from one or more of these screening methods, they need to be thoroughly characterized in order to con?rm activity and identify areas in need of optimization. Finally, once fully characterized hits are identi?ed, preliminary optimization through synthetic modi?cation is carried out to generate leads. Parallel optimization of all properties, including biological, physicochemical, and ADME is the most ef?cient approach to the identi?cation of leads. Hit characterization is described in the previous chapter. The focus of this chapter is on hit optimization and the identi?- tion of leads. After a general overview of these processes, examples taken from the literature since 2001 will be used to illustrate speci?c points. There are also a number of excellent reviews covering the lead identi?cation process [1–6].
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.
Book Synopsis Towards Drugs of the Future by : Chris G. Kruse
Download or read book Towards Drugs of the Future written by Chris G. Kruse and published by IOS Press. This book was released on 2008 with total page 140 pages. Available in PDF, EPUB and Kindle. Book excerpt: "The ninth Solvay Pharmaceutical Conference on Medicinal Chemistry held in Garmisch-Partenkirchen (Germany) September 26-28, 2007"--P. vi.
Book Synopsis Lead Generation, 2 Volume Set by : Jörg Holenz
Download or read book Lead Generation, 2 Volume Set written by Jörg Holenz and published by John Wiley & Sons. This book was released on 2016-06-27 with total page 818 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.
Book Synopsis Small Molecule Medicinal Chemistry by : Werngard Czechtizky
Download or read book Small Molecule Medicinal Chemistry written by Werngard Czechtizky and published by John Wiley & Sons. This book was released on 2015-09-21 with total page 528 pages. Available in PDF, EPUB and Kindle. Book excerpt: Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting
Book Synopsis High-Throughput Lead Optimization in Drug Discovery by : Tushar Kshirsagar
Download or read book High-Throughput Lead Optimization in Drug Discovery written by Tushar Kshirsagar and published by CRC Press. This book was released on 2008-03-04 with total page 256 pages. Available in PDF, EPUB and Kindle. Book excerpt: A Single Source on Parallel Synthesis for Lead Optimization The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high qualit
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.
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 Academic Press. This book was released on 2011-05-02 with total page 982 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Optimizing the "Drug-Like" Properties of Leads in Drug Discovery by : Ronald Borchardt
Download or read book Optimizing the "Drug-Like" Properties of Leads in Drug Discovery written by Ronald Borchardt and published by Springer Science & Business Media. This book was released on 2007-12-31 with total page 522 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book arises from a workshop organized by the American Association of Pharmaceutical Scientists entitled "Optimizing the Drug-Like Properties of Leads in Drug Discovery," which took place in Parsippany, NJ in September 2004. The workshop focused on the optimization of the drug-like properties of leads in drug discovery. The volume outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process.
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.
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.
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.
Book Synopsis Towards Drugs of the Future by : Chris G. Kruse
Download or read book Towards Drugs of the Future written by Chris G. Kruse and published by . This book was released on 2008 with total page 129 pages. Available in PDF, EPUB and Kindle. Book excerpt: The scope of this book is that the pharmaceutical industry must change the way it operates. The editors of this book feel that the current business model is economically unsustainable and incapable to meet expectations of modern society. The number of novel medications in the global industry pipeline is insufficient to suffice demand of the markets, the financial performance of several companies is declining, sales and marketing costs are rising, regulatory constraints are increasingly challenging and overall reputation of industry is tarnishing. Unmet medical needs must be better addressed and tangible benefits need to be exposed in order to be rewarded by healthcare payers. In addition, the focus is shifting from simple treatment of the ill to preventative measures and health management. This volume addresses newest development in synthetic and medicinal chemistry with the emphasis on global challenges.
Book Synopsis Hit and Lead Profiling by : Bernard Faller
Download or read book Hit and Lead Profiling written by Bernard Faller and published by Wiley-VCH. This book was released on 2009-09-28 with total page 533 pages. Available in PDF, EPUB and Kindle. Book excerpt: The only reference on current methods to generate pharmacokinetic and safety profiles of drug candidates, as well as how they must be balanced against one other for the best selection of candidates for further development. Following a brief introduction to the necessities of filtering and risk assessment of potential new drug molecules before actual drug development, the two equally important aspects of pharmacological (ADME) and safety (toxicity) profiling are covered in separate parts. The ADME section covers the profiling of basic physicochemical parameters, such as solubility and permeability, as well as more complex traits, such as the likelihood of drug-drug interactions, metabolic clearance and protein binding properties. The toxicology part addresses, among others, recent advances in early genetic toxicity testing, bioactivation screening, organ-specific toxicity assays for liver, heart, kidney and blood, as well as profiling for autoimmune reactions. By addressing both drug efficiency and drug safety, this modern practical reference shows readers how each individual aspect figures in shaping the key decisions on which the entire drug development process hinges. In short, this is a complete toolbox for assessing the risk/benefit ratio for any novel compound during the early drug development stages, using both in vitro and in silico methods. Both editors are based at one of the leading research-driven pharmaceutical companies, and the authors have been recruited from numerous other global players in the field. Invaluable know-how for every medicinal chemist and drug developer.
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 Elsevier. This book was released on 2003-06-11 with total page 792 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Reducing Drug Attrition by : James R. Empfield
Download or read book Reducing Drug Attrition written by James R. Empfield and published by Springer. This book was released on 2014-11-27 with total page 176 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
