Piperidine Based Drug Discovery PDF Download
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Author | : Ruben Vardanyan |
Publisher | : Elsevier |
Total Pages | : 359 |
Release | : 2017-06-12 |
Genre | : Science |
ISBN | : 0128134283 |
Download Piperidine-Based Drug Discovery Book in PDF, ePub and Kindle
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
Author | : Larry Yet |
Publisher | : John Wiley & Sons |
Total Pages | : 560 |
Release | : 2018-03-27 |
Genre | : Medical |
ISBN | : 1118145666 |
Download Privileged Structures in Drug Discovery Book in PDF, ePub and Kindle
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 | : Jie Jack Li |
Publisher | : CRC Press |
Total Pages | : 320 |
Release | : 2021-10-21 |
Genre | : Medical |
ISBN | : 1000416011 |
Download Drug Discovery with Privileged Building Blocks Book in PDF, ePub and Kindle
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.
Author | : Arun K. Ghosh |
Publisher | : John Wiley & Sons |
Total Pages | : 474 |
Release | : 2014-08-11 |
Genre | : Medical |
ISBN | : 3527333657 |
Download Structure-based Design of Drugs and Other Bioactive Molecules Book in PDF, ePub and Kindle
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.
Author | : Steven Howard |
Publisher | : Royal Society of Chemistry |
Total Pages | : 314 |
Release | : 2015-06-17 |
Genre | : Medical |
ISBN | : 1782625658 |
Download Fragment-Based Drug Discovery Book in PDF, ePub and Kindle
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.
Author | : Ernst Jucker |
Publisher | : Springer Science & Business Media |
Total Pages | : 314 |
Release | : 1999 |
Genre | : Drugs |
ISBN | : 9783764360283 |
Download Progress in Drug Research Book in PDF, ePub and Kindle
Progress in Drug Research is a prestigious book series which provides extensive expert-written reviews on a wide spectrum of highly topical areas in current pharmaceutical and pharmacological research. It serves as an important source of information for researchers concerned with drug research and all those who need to keep abreast of the many recent developments in the quest for new and better medicines.
Author | : János Fischer |
Publisher | : John Wiley & Sons |
Total Pages | : 258 |
Release | : 2015-05-04 |
Genre | : Medical |
ISBN | : 3527336850 |
Download Successful Drug Discovery, Volume 1 Book in PDF, ePub and Kindle
The first volume of the book series "Successful Drug Discovery" is focusing on new drug discoveries during the last decade, from established drugs to recently introduced drugs of all kinds: small-molecule-, peptide-, and protein-based drugs. The role of serendipity is analyzed in some very successful drugs where the research targets of the lead molecule and the drug are different. Phenotypic and target-based drug discovery approaches are discussed from the viewpoint of pioneer drugs and analogues. This volume gives an excellent overview of insulin analogues including a discussion of the properties of rapid-acting and long-acting formulations of this important hormone. The major part of the book is devoted to case histories of new drug discoveries described by their key inventors. Eight case histories range across many therapeutic fields. The goal of this book series is to help the participants of the drug research community with a reference book series and to support teaching in medicinal chemistry with case histories and review articles of new drugs.
Author | : Barry A. Bunin |
Publisher | : Elsevier |
Total Pages | : 341 |
Release | : 1998-04-15 |
Genre | : Science |
ISBN | : 0080542409 |
Download The Combinatorial Index Book in PDF, ePub and Kindle
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
Author | : Stefan Bräse |
Publisher | : Royal Society of Chemistry |
Total Pages | : 486 |
Release | : 2015-11-20 |
Genre | : Medical |
ISBN | : 1782620303 |
Download Privileged Scaffolds in Medicinal Chemistry Book in PDF, ePub and Kindle
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Author | : Pandi Veerapandian |
Publisher | : Routledge |
Total Pages | : 665 |
Release | : 2018-03-29 |
Genre | : Medical |
ISBN | : 1351413066 |
Download Structure-Based Drug Design Book in PDF, ePub and Kindle
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!