Synthetic Methods In Drug Discovery

Author : David C. Blakemore,Paul M. Doyle,Yvette M. Fobian
Publisher : Royal Society of Chemistry
Page : 474 pages
File Size : 49,7 Mb
Release : 2016
Category : Drug development
ISBN : 9781849738033

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Synthetic Methods in Drug Discovery by David C. Blakemore,Paul M. Doyle,Yvette M. Fobian Pdf

The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.

Author : David Blakemore,Yvette Fobian,Paul Doyle
Publisher : Drug Discovery
Page : 0 pages
File Size : 45,6 Mb
Release : 2016-08
Category : Science
ISBN : 1782627871

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Synthetic Methods in Drug Discovery by David Blakemore,Yvette Fobian,Paul Doyle Pdf

Author : David C. Blakemore,Paul M. Doyle,Yvette M. Fobian
Publisher : Royal Society of Chemistry
Page : 536 pages
File Size : 43,6 Mb
Release : 2016
Category : Drug development
ISBN : 9781782627869

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Synthetic Methods in Drug Discovery by David C. Blakemore,Paul M. Doyle,Yvette M. Fobian Pdf

The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.

Author : Elizabeth Farrant
Publisher : Royal Society of Chemistry
Page : 176 pages
File Size : 43,9 Mb
Release : 2011-10-04
Category : Medical
ISBN : 9781849733052

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New Synthetic Technologies in Medicinal Chemistry by Elizabeth Farrant Pdf

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.

Author : Andrea Trabocchi,Elena Lenci
Publisher : Elsevier
Page : 358 pages
File Size : 53,8 Mb
Release : 2019-11-23
Category : Science
ISBN : 9780128183502

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Small Molecule Drug Discovery by Andrea Trabocchi,Elena Lenci Pdf

Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules

Author : Vasyl Andrushko,Natalia Andrushko
Publisher : John Wiley & Sons
Page : 1836 pages
File Size : 51,9 Mb
Release : 2013-08-16
Category : Science
ISBN : 9781118628331

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Stereoselective Synthesis of Drugs and Natural Products by Vasyl Andrushko,Natalia Andrushko Pdf

Brings together the best tested and proven stereoselective synthetic methods Both the chemical and pharmaceutical industries are increasingly dependent on stereoselective synthetic methods and strategies for the generation of new chiral drugs and natural products that offer specific 3-D structures. With the publication of Stereoselective Synthesis of Drugs and Natural Products, researchers can turn to this comprehensive two-volume work to guide them through all the core methods for the synthesis of chiral drugs and natural products. Stereoselective Synthesis of Drugs and Natural Products features contributions from an international team of synthetic chemists and pharmaceutical and natural product researchers. These authors have reviewed the tremendous body of literature in the field in order to compile a set of reliable, tested, and proven methods alongside step-by-step guidance. This practical resource not only explores synthetic methodology, but also reaction mechanisms and applications in medicinal chemistry and drug discovery. The publication begins with an introductory chapter covering general principles and methodologies, nomenclature, and strategies of stereoselective synthesis. Next, it is divided into three parts: Part One: General Methods and Strategies Part Two: Stereoselective Synthesis by Bond Formation including C-C bond formation C-H bond formation C-O bond formation C-N bond formation Other C-heteroatom formation and other bond formation Part Three: Methods of Analysis and Chiral Separation References in every chapter serve as a gateway to the literature in the field. With this publication as their guide, chemists involved in the stereoselective synthesis of drugs and natural products now have a single, expertly edited source for all the methods they need.

Author : Jie Jack Li,Douglas S. Johnson
Publisher : John Wiley & Sons
Page : 358 pages
File Size : 52,8 Mb
Release : 2015-12-14
Category : Science
ISBN : 9781118820056

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Innovative Drug Synthesis by Jie Jack Li,Douglas S. Johnson Pdf

This book covers all aspects of the medicinal chemistry of the latest drugs, and the cutting-edge science associated with them. Following the editors’ 3 successful drug synthesis books, this provides expert analysis of the pros and cons of different synthetic routes and demystifies the process of modern drug discovery for practitioners and researchers. Summarizes for each drug: respective disease area, important properties and SAR (structure-activity relationship), and chemical synthesis routes / options Includes case studies in each chapter Illustrates how chemistry, biology, pharmacokinetics, and a host of disciplines come together to produce successful medicines Explains the advantages of process synthesis versus the synthetic route for drug discovery

Author : Larry Yet
Publisher : John Wiley & Sons
Page : 560 pages
File Size : 41,6 Mb
Release : 2018-03-27
Category : Medical
ISBN : 9781118145661

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Privileged Structures in Drug Discovery by Larry Yet Pdf

A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.

Author : James Kyranos
Publisher : Elsevier
Page : 204 pages
File Size : 50,6 Mb
Release : 2004-09-18
Category : Science
ISBN : 9780080472928

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High Throughput Analysis for Early Drug Discovery by James Kyranos Pdf

High Throughput Analysis for Early Drug Discovery offers concise and unbiased presentations by synthetic and analytical chemists who have been involved in creating and moving the field of combinatorial chemistry into the academic and industrial mainstream. Since the synthetic method often dictates the appropriate types of analysis, each chapter or section begins with a description of the synthesis approach and its advantages. The description of various combinatorial and high-throughput parallel synthesis techniques provide a relevant point of entry for synthetic chemists who need to set up appropriate characterisation methods for his/her organisation. This is an invaluable resource for all organic and analytical chemists in the pharmaceutical, agrochemical, and biotechnology fields who are either involved in, or beginning to investigate combinatorial techniques to increase overall efficiency and productivity. First reference to focus on the analytical side of synthesis

Author : Jie Jack Li
Publisher : John Wiley & Sons
Page : 720 pages
File Size : 47,6 Mb
Release : 2013-04-26
Category : Science
ISBN : 9781118354438

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Heterocyclic Chemistry in Drug Discovery by Jie Jack Li Pdf

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.

Author : Vasyl Andrushko,Natalia Andrushko
Publisher : Wiley
Page : 0 pages
File Size : 53,9 Mb
Release : 2013-10-07
Category : Science
ISBN : 1118032179

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Stereoselective Synthesis of Drugs and Natural Products, 2 Volume Set by Vasyl Andrushko,Natalia Andrushko Pdf

Brings together the best tested and proven stereoselective synthetic methods Both the chemical and pharmaceutical industries are increasingly dependent on stereoselective synthetic methods and strategies for the generation of new chiral drugs and natural products that offer specific 3-D structures. With the publication of Stereoselective Synthesis of Drugs and Natural Products, researchers can turn to this comprehensive two-volume work to guide them through all the core methods for the synthesis of chiral drugs and natural products. Stereoselective Synthesis of Drugs and Natural Products features contributions from an international team of synthetic chemists and pharmaceutical and natural product researchers. These authors have reviewed the tremendous body of literature in the field in order to compile a set of reliable, tested, and proven methods alongside step-by-step guidance. This practical resource not only explores synthetic methodology, but also reaction mechanisms and applications in medicinal chemistry and drug discovery. The publication begins with an introductory chapter covering general principles and methodologies, nomenclature, and strategies of stereoselective synthesis. Next, it is divided into three parts: Part One: General Methods and Strategies Part Two: Stereoselective Synthesis by Bond Formation including C-C bond formation C-H bond formation C-O bond formation C-N bond formation Other C-heteroatom formation and other bond formation Part Three: Methods of Analysis and Chiral Separation References in every chapter serve as a gateway to the literature in the field. With this publication as their guide, chemists involved in the stereoselective synthesis of drugs and natural products now have a single, expertly edited source for all the methods they need.

Author : Emily A. Peterson,Julie B. Manley
Publisher : Royal Society of Chemistry
Page : 338 pages
File Size : 47,5 Mb
Release : 2015-06-30
Category : Medical
ISBN : 9781849739610

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Green Chemistry Strategies for Drug Discovery by Emily A. Peterson,Julie B. Manley Pdf

The incorporation of Green Chemistry is a relatively new phenomenon in the drug discovery discipline, since the scale that chemists operate on in drug discovery is smaller than those of process and manufacturing chemistry. The necessary metrics are more difficult to obtain in drug discovery due to the diversity of reactions conducted. However, pharmaceutical companies are realizing that incorporation of green chemistry techniques at earlier stages of drug development can speed the development of a drug candidate. Edited by experts who have pioneered green chemistry efforts within their own institutions, this book provides a practical guide for both academic and industrial labs wanting to know where to start with introducing greener approaches for greatest return on investment. The Editors have taken a comprehensive approach to the topic covering the entire drug discovery process from molecule conception, through synthesis, formulation and toxicology with specific examples and case studies where green chemistry strategies have been implemented. Currently employed as well as emerging techniques for performing greener drug discovery chemistry are addressed as well as cutting-edge topics like biologics discovery. Moreover, important surrounding issues such as intellectual property are included. This book will serve as a practical guide for both academic and industrial chemists who work across the breadth of the drug discovery discipline. Ultimately, readers will learn how to incorporate green chemistry strategies into their everyday workflow without slowing down their science.

Author : Stefan Bräse
Publisher : Royal Society of Chemistry
Page : 486 pages
File Size : 48,7 Mb
Release : 2015-11-20
Category : Medical
ISBN : 9781782620303

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Privileged Scaffolds in Medicinal Chemistry by Stefan Bräse Pdf

This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Author : F. Gualtieri
Publisher : Wiley-VCH
Page : 382 pages
File Size : 53,5 Mb
Release : 2000-03-22
Category : Science
ISBN : UOM:39015050308777

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New Trends in Synthetic Medicinal Chemistry, Volume 7 by F. Gualtieri Pdf

The long-awaited volume on synthetic chemistry in the series "Methods and Principles in Medicinal Chemistry" is now available. In the pharmaceutical industry, computational methods play a major role in the discovery and development of new drugs. Yet, the SYNTHESIS of these compounds still remains the most crucial topic in drug design. Written by an internationally renowned team of authors and editors from academia and industry, this volume describes all recent developments in organic synthetic methodology which are essential for pharmaceutical research. The most modern synthetic developments of pharmacologically interesting compounds (carbohydrates and nucleotides) as well as important synthetic methods such as combinatorial chemistry, solid-phase reactions, bioassisted organic synthesis and asymmetric synthesis are critically discussed. Special emphasis is given to a hands-on practical approach which enables researchers to apply the featured methods immediately to their specific problems. Also, the detailed presentation of the topic and the selection of references will be of help to any researcher working in the laboratory.

Author : C. Brown
Publisher : Academic Press
Page : 243 pages
File Size : 53,9 Mb
Release : 2013-10-22
Category : Medical
ISBN : 9781483288246

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Chirality in Drug Design and Synthesis by C. Brown Pdf

Chirality in Drug Design and Synthesis is a collection of papers that discusses the property of asymmetry in the structural and synthetic chemistry of natural products, including the significance of chirality in medicinal chemistry. These papers examine the need for the preparation and study of pure enantiomers of chiral drug substances and their mechanism of interaction with enzymes and receptors. These papers also investigate the techniques in studying these interactions, as well as analyze the methods for their synthesis in enantiomerically pure form. One paper discusses the pharmacological and pharmacokinetic analyses made that point to the differences in the activity and disposition of enantiometric pairs. Another paper reviews the implications of the neglect of stereoselectivity at the different levels during the examination process of racemic drugs. Since no general guidelines exists for the development of drugs with chiral centers, one paper suggests a case-by-case approach in evaluating the safety and efficacy of drugs, particularly as regards how isomers differ in their effects. This collection is suitable for the pharmacologist, medicinal chemists, toxicologists, mechanistic chemists and synthetic organic chemists.