Download or read book Piperidine Based Drug Discovery written by Ruben Vardanyan and published by Elsevier. This book was released on 2017-06-12 with total page 359 pages. Available in PDF, EPUB and Kindle. Book excerpt: Piperidine-Based Drug Discovery outlines the complexities of Piperidine scaffold use in drug discovery, including derivative chemistry, structural properties, methods of synthesis and practical implementations. Piperidine scaffolds are the cornerstones of over 70 commercialized drugs (including multiple blockbusters). Designed as a guide for both experts and students working in this and related areas, it is hoped that this volume will encourage and inspire the continued design and development of novel pharmaceuticals based on Piperidine and its derivatives. Heterocyclic compounds are of central importance to medicinal chemistry, as demonstrated by the high percentage of marketable drugs that feature heterocyclic fragments in their structures. As starting points for drug discovery they offer a broad range of attractive properties, and a detailed understanding of the particular characteristics of each is of great benefit to researchers. The most commonly used heterocycle among US FDA approved pharmaceuticals, Piperidine is an extremely important building block in the synthesis of medicinal agents. This heterocycle and its derivatives exhibit a number of important functionalities and have been employed variously as CNS modulators, antiaggregants, anticoagulants, antihistamines, anti-cancer drugs and analgesics. Explores this extremely important heterocycle to a high level of detail Describes synthesis methods for 70 current drugs based on Piperidine scaffolds Gives drug designers all the key knowledge required to develop new drugs utilizing Piperidine Provides pharmacologists a solid overview of the chemical background of existing Piperidine-based drugs

Download or read book Drug Discovery with Privileged Building Blocks written by Jie Jack Li and published by CRC Press. This book was released on 2021-10-21 with total page 320 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug Discovery with Privileged Building Blocks traces back PharmaBlock’s founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book. Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well. Key Feature The book covers privileged building blocks appearing most frequently on patents for novel drugs. The latest relevant tactics are explained in the context of drug design and medicinal chemistry. Key synthesis, especially large-scale synthesis, is described. The most recent literature references are cited.

Download or read book Privileged Structures in Drug Discovery written by Larry Yet and published by John Wiley & Sons. This book was released on 2018-03-07 with total page 562 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Download or read book Progress in Drug Research written by and published by Birkhäuser. This book was released on 2012-12-06 with total page 287 pages. Available in PDF, EPUB and Kindle. Book excerpt: Hypertension is one of the cardiovascular diseases which is most common throughout the world. It is generally defined as an elevation of systolic and/or diastolic arterial blood pressure, which is 120/80 mm Hg in normal situation. A value of 140/90 mm is generally accepted as the upper limit of normotension. Hypertension with certain risk factors such as hypercholes terolemia, diabetes, smoking and a family history of vascular disease pre disposes to arteriosclerosis and consequent cardiovascular morbidity and mortality. The treatment of hypertension leads to reduced risk of hyperten sive renal failure, haemorrhagic stroke, myocardial infarction and cardiac failure. In most cases, the cause of the hypertension can not be clearly defined. Such hypertension is termed as essential hypertension. In a few cases (5- 15%), the hypertension is secondary to definable causes, such as renal artery stenosis, a pheochromocytoma, or an endocrine disorder. This type of hyper tension is known as secondary hypertenSion. Although the exact etiology of essential hypertension is still not well known, the following factors are sup posed to play causative roles.

Download or read book Anti Inflammatory Drug Discovery written by Jeremy I. Levin and published by Royal Society of Chemistry. This book was released on 2012 with total page 545 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive review of recent medicinal chemistry approaches to a variety of important therapeutic targets and a key reference for those interested in the prosecution of modern drug discovery programs directed at anti-inflammatory mechanisms of action.

Download or read book Chemokines written by Nuska Tschammer and published by Springer. This book was released on 2015-03-02 with total page 248 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.

Download or read book Structure based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

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.

Download or read book Progress in Medicinal Chemistry written by F.D. King and published by Gulf Professional Publishing. This book was released on 2005-06-14 with total page 312 pages. Available in PDF, EPUB and Kindle. Book excerpt: Annotation The complex and multidisciplinary nature of modern drug discovery is well illustrated in the six chapters of this volume that describe exciting developments in both newly emerging and mature areas of medicinal chemistry. Chapter 1 provides a comprehensive review of therapeutic applications of ligands for peroxisome proliferator-activated receptor gamma PPAR?, a key regulator of glucose and lipid homeostasis. Progress over the last decade on ligands that bind to central nicotinic acetylcholine receptors is timely reviewed in Chapter 2, with the emphasis on the a4ß2 subtype. Chapter 3 reviews inhibitors of PARP-1, the founding member of the family, with the focus on their therapeutic potential in ischaemia related CNS injuries. Chapter 4 describes the structure-activity relationships of some semi-synthetic analogues including promising new compounds in development. Chapter 5 describes selective, first generation, non-peptidic neuropeptide Y1 and Y2 antagonists and their actions and evaluates their potential therapeutic application in cardiovascular disorders, with the emphasis on NPY1 antagonists. Chapter 6 is an extensive review of the considerable progress that has been achieved in developing Cathepsin K inhibitors and evaluates their potential for treating arthritis and atherosclerosis.

Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Download or read book The Combinatorial Index written by Barry A. Bunin and published by Elsevier. This book was released on 1998-04-15 with total page 341 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods Serves as a laboratory manual for bench chemists Includes a chapter on linkers to assist in choice of linking strategy Discusses strengths and limitations of the various methods Contains a structural index showing functional group transformations in solid-phase synthesis

Download or read book Fragment based Approaches in Drug Discovery written by Wolfgang Jahnke and published by John Wiley & Sons. This book was released on 2006-12-13 with total page 391 pages. Available in PDF, EPUB and Kindle. Book excerpt: This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.

Download or read book Structure Based Drug Design written by Pandi Veerapandian and published by Routledge. This book was released on 2018-03-29 with total page 665 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introducing the most recent advances in crystallography, nuclear magnetic resonance, molecular modeling techniques, and computational combinatorial chemistry, this unique, interdisciplinary reference explains the application of three-dimensional structural information in the design of pharmaceutical drugs. Furnishing authoritative analyses by world-renowned experts, Structure-Based Drug Design discusses protein structure-based design in optimizing HIV protease inhibitors and details the biochemical, genetic, and clinical data on HIV-1 reverse transcriptase presents recent results on the high-resolution three-dimensional structure of the catalytic core domain of HIV-1 integrase as a foundation for divergent combination therapy focuses on structure-based design strategies for uncovering receptor antagonists to treat inflammatory diseases demonstrates a systematic approach to the design of inhibitory compounds in cancer treatment reviews current knowledge on the Interleukin-1 (IL-1) system and progress in the development of IL-1 modulators describes the influence of structure-based methods in designing capsid-binding inhibitors for relief of the common cold and much more!

Download or read book Pyridines From Lab to Production written by Eric F.V. Scriven and published by Academic Press. This book was released on 2013-01-08 with total page 583 pages. Available in PDF, EPUB and Kindle. Book excerpt: Pyridines: From Lab to Production provides a synthetic armory of tools to aid the practicing chemist by reviewing the most reliable historical methods alongside new methods/ Written by scientists who have actually used these in synthesis. By emphasizing tricks and tips to optimize reactions for the best yields and purity, which are often missing from the primary literature, this book provides another dimension for the synthetic chemist. A combined academic and industrial approach evaluates the best methods for different scales of reaction and discusses practical tips (e.g. when to stop a reaction early to maximize purity or when to re-use side products). Chapters also assess whether to make or source starting materials, how to connect them and what are the best synthetic routes. The book is designed to be a stand-alone reference, but also provides cross references to leading reviews and the Comprehensive Heterocyclic Chemistry reference works for those who want to learn more. Reviews tried and tested practical methods to help the reader select the best method for their research Includes tips, tricks and hints to enable the reader to get the best yield or cleanest product out of their reaction for synthesising or transforming a pyridine derivative Written by both academic researchers and industry leaders this provides a unique view of how to get the most out of a reaction no matter what scale you are running this on

Download or read book Copper in N Heterocyclic Chemistry written by Ananya Srivastava and published by Elsevier. This book was released on 2020-11-13 with total page 506 pages. Available in PDF, EPUB and Kindle. Book excerpt: Copper in N-Heterocyclic Chemistry provides an overview of copper-catalyzed synthesis and functionalization of N-heterocyclic compounds, covering all recent developments in a way that is ideal for researchers and students working in the area of synthetic organic chemistry and medicinal chemistry. The book explores N-heterocyclic compounds as unique structural units in the development of natural products and pharmaceuticals, along with the remarkable progress made in the area of high atom economic strategies, and more recently, copper-catalyzed C-H activation and its applications in organic synthesis. Readers will find troubleshooting protocols, as well as the advantages and limitations of each method discussed. As copper catalysts show versatile chemical reactivity in many aspects, including their oxidation states 0–3 are accessible and their ability to facilitate bond formations due to their ability to serve as Lewis acids, oxidizing agents and catalysts, this book is an ideal resource on the topics explored. Discusses novel synthetic methods developed over the past decade for copper-catalyzed synthesis of N-heterocyclic compounds Covers the most recent methodologies adapted in synthetic chemistry for applications in natural products and pharmaceuticals Includes troubleshooting protocols, as well as the advantages and limitations of each method discussed in detail

Download or read book Peptidomimetics in Organic and Medicinal Chemistry written by Antonio Guarna and published by John Wiley & Sons. This book was released on 2014-04-07 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins