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Piperidine-Based Drug Discovery

Piperidine-Based Drug Discovery
A Book

by Ruben Vardanyan

  • Publisher : Elsevier
  • Release : 2017-06-12
  • Pages : 358
  • ISBN : 0128134283
  • Language : En, Es, Fr & De
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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

Fragment-based Drug Discovery

Fragment-based Drug Discovery
Lessons and Outlook

by Daniel A. Erlanson,Wolfgang Jahnke,Raimund Mannhold,Hugo Kubinyi,Gerd Folkers

  • Publisher : John Wiley & Sons
  • Release : 2016-02-23
  • Pages : 528
  • ISBN : 352733775X
  • Language : En, Es, Fr & De
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From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.

Green Sustainable Process for Chemical and Environmental Engineering and Science

Green Sustainable Process for Chemical and Environmental Engineering and Science
Solvents for the Pharmaceutical Industry

by Dr. Inamuddin,Rajender Boddula,Mohd Imran Ahamed,Abdullah M. Asiri

  • Publisher : Elsevier
  • Release : 2020-12-01
  • Pages : 374
  • ISBN : 0128218991
  • Language : En, Es, Fr & De
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Green Sustainable Process for Chemical and Environmental Engineering and Science: Solvents for the Pharmaceutical Industry aims at providing a detailed overview of applications of green solvents in pharmaceutical industries. It also focuses on providing a detailed literature survey on the green solvents for pharmaceutical analysis, drug design, synthesis, and production, etc. It summarizes the applications of various greens solvents such as water, cyrene, vegetable oils, ionic liquids, ethyl lactate, eutectic solvents, and glycerol in contrast to toxic solvents. This book provides an overview of the use of green solvents for the sustainable and environmentally friendly development of synthetic methodologies for biomedical and pharmaceutical industries. Up-to-date developments towards the development of solvents for pharmaceutical industry Includes latest advances in pharmaceutical analysis and synthesis using green solvents Outlines eco-friendly green solvents for medicinal applications State-of-the-art overview on the exploration of green solvents for pharmaceutical industries

Carbohydrate-based Drug Discovery

Carbohydrate-based Drug Discovery
A Book

by Chi-Huey Wong

  • Publisher : Wiley-VCH
  • Release : 2003-10-17
  • Pages : 980
  • ISBN : 9783527306329
  • Language : En, Es, Fr & De
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To exploit the full potential of this diverse compound class for the development of novel active substances, this handbook presents the latest knowledge on carbohydrate chemistry and biochemistry. While it is unique in covering the entire field, particular emphasis is placed on carbohydrates with pharmaceutical potential. Topics include the following:br” Chemical Synthesis of Carbohydratesbr” Carbohydrate Biosynthesis and Metabolism

Antiviral Drugs

Antiviral Drugs
From Basic Discovery Through Clinical Trials

by Wieslaw M. Kazmierski

  • Publisher : John Wiley & Sons
  • Release : 2011-07-08
  • Pages : 472
  • ISBN : 0470934689
  • Language : En, Es, Fr & De
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This book focuses on new small molecule approaches to combat viral infections. The chapters describe the discovery and development from bench through the clinic of relatively recently-approved antiviral drugs and compounds in advanced clinical development. Organized by a virus (such as HIV, HCV, RSV, influenza, HBV and CMV) and written by top academic and industrial authorities in the field, the book provides a unique opportunity to study, understand and apply discovery and development principles and learning without the need for an individual to research, analyze and synthesize all immense sourcing references. Topics showcase challenges and solutions of issues encountered, offering tremendous experience accumulated over many years of research that will be particularly useful to basic and bench scientists as well as clinicians as they continue discovering and developing new drugs and therapies.

Structure-based Design of Drugs and Other Bioactive Molecules

Structure-based Design of Drugs and Other Bioactive Molecules
Tools and Strategies

by Arun K. Ghosh,Sandra Gemma

  • Publisher : John Wiley & Sons
  • Release : 2014-08-11
  • Pages : 474
  • ISBN : 3527333657
  • Language : En, Es, Fr & De
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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.

Synthesis of Best-Seller Drugs

Synthesis of Best-Seller Drugs
A Book

by Ruben Vardanyan,Victor Hruby

  • Publisher : Academic Press
  • Release : 2016-01-07
  • Pages : 868
  • ISBN : 0124115241
  • Language : En, Es, Fr & De
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Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation

Multicomponent Reactions

Multicomponent Reactions
Synthesis of Bioactive Heterocycles

by K.L. Ameta, Ph.D.,Anshu Dandia

  • Publisher : CRC Press
  • Release : 2017-09-20
  • Pages : 394
  • ISBN : 1315352737
  • Language : En, Es, Fr & De
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This timely book provides a succinct summary of methods for the synthesis of bioactive heterocycles using a multicomponent reaction (MCR) approach. The majority of pharmaceuticals and biologically active agrochemicals are heterocycles while countless additives and modifiers used in industrial applications are heterocyclic in nature. With the recent introduction of high-throughput biological evaluation, the importance of MCRs for drug discovery has been recognized and considerable efforts have been focused especially on the design and development of multi-component procedures for the generation of various bioactive heterocycles due to their significant therapeutic potential.

Pyridine

Pyridine
A Book

by Pratima Parashar Pandey

  • Publisher : BoD – Books on Demand
  • Release : 2018-07-18
  • Pages : 84
  • ISBN : 1789234220
  • Language : En, Es, Fr & De
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This book is designed and styled in order to give researchers a vast horizon about pyridine. A deep look in the structural analysis of pyridine provides a base for all the building blocks derived from it and its applications. Pyridines and pyridine moieties are found in many natural products, such as vitamins, coenzymes, alkaloids, many drugs, and pesticides. The book is divided into three parts: the first takes to the introduction, the second part deals with composition of various compounds using heterocyclic ring of pyridine, and the third part discusses about applications of pyridine compounds.

Structure-Function Analysis of G Protein-Coupled Receptors

Structure-Function Analysis of G Protein-Coupled Receptors
A Book

by Jürgen Wess

  • Publisher : Wiley-Liss
  • Release : 1999-06-15
  • Pages : 440
  • ISBN : 9780471252283
  • Language : En, Es, Fr & De
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G protein-coupled receptors (GPCRs) are the largest single class of receptors in biology, often playing key roles in a remarkably large number of physiological and pathophysiological conditions. GPCRs or GPCR-dependent signalling pathways are the targets of a very large number of therapeutically useful drugs. Detailed knowledge about the molecular structure of GPCRs should therefore pave the way for the design of novel drugs with increased efficacy and specificity. This volume provides a concise, up-to-date presentation of methods (including molecular genetic, biochemical, and biophysical) which have been used successfully in studying the structure and function of GPCRs. With contributions from international leaders in the field, the editor provides overviews of various techniques, followed by in-depth descriptions of basic procedures and discussions of critical experimental parameters. Divided into specific, accessible sections, Structure-Function Analysis of G Protein-Coupled Receptors includes: * An overview of mutagenesis techniques * Examples of molecular modeling techniques * Using peptides as tools for the study of GPCR interactions * Site-Directed Spin Labeling (SDSL) studies of the GPCR rhodopsin * A complete description of the electron-crystalographic analysis of two-dimensional rhodopsin crystals * The use of nuclear magnetic resonance techniques to study GPCR structure

Synthesis of Essential Drugs

Synthesis of Essential Drugs
A Book

by Ruben Vardanyan,Victor Hruby

  • Publisher : Elsevier
  • Release : 2006-03-10
  • Pages : 634
  • ISBN : 9780080462127
  • Language : En, Es, Fr & De
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Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO’s Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types * Includes synonyms * Includes over 2300 references

Methods and Techniques in Drug Discovery

Methods and Techniques in Drug Discovery
A Book

by John Sterling,Ellyn J. T. D. Kerr,Shannon Simons

  • Publisher : Unknown Publisher
  • Release : 2005
  • Pages : 266
  • ISBN : 9876543210XXX
  • Language : En, Es, Fr & De
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HIV-1 Integrase

HIV-1 Integrase
Mechanism and Inhibitor Design

by Nouri Neamati

  • Publisher : John Wiley & Sons
  • Release : 2011-08-10
  • Pages : 520
  • ISBN : 1118015363
  • Language : En, Es, Fr & De
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This book comprehensively covers the mechanisms of action and inhibitor design for HIV-1 integrase. It serves as a resource for scientists facing challenging drug design issues and researchers in antiviral drug discovery. Despite numerous review articles and isolated book chapters dealing with HIV-1 integrase, there has not been a single source for those working to devise anti-AIDS drugs against this promising target. But this book fills that gap and offers a valuable introduction to the field for the interdisciplinary scientists who will need to work together to design drugs that target HIV-1 integrase.

Fragment-based Approaches in Drug Discovery

Fragment-based Approaches in Drug Discovery
A Book

by Wolfgang Jahnke,Daniel A. Erlanson

  • Publisher : John Wiley & Sons
  • Release : 2006-12-13
  • Pages : 391
  • ISBN : 3527608605
  • Language : En, Es, Fr & De
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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.

Fragment-based Approaches in Drug Discovery

Fragment-based Approaches in Drug Discovery
A Book

by Wolfgang Jahnke,Daniel A. Erlanson

  • Publisher : John Wiley & Sons
  • Release : 2006-12-13
  • Pages : 391
  • ISBN : 3527608605
  • Language : En, Es, Fr & De
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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.

Diversity Oriented Synthesis

Diversity Oriented Synthesis
A Book

by Andrea Basso,Seung Bum Park,Lisa Moni

  • Publisher : Frontiers Media SA
  • Release : 2019-03-22
  • Pages : 329
  • ISBN : 2889457885
  • Language : En, Es, Fr & De
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Has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade.

Peptides as Drugs

Peptides as Drugs
Discovery and Development

by Bernd Groner

  • Publisher : John Wiley & Sons
  • Release : 2009-11-18
  • Pages : 242
  • ISBN : 3527626840
  • Language : En, Es, Fr & De
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By covering the full spectrum of topics relevant to peptidic drugs, this timely handbook serves as an introductory reference for both drug developers and biomedical researchers interested in pharmaceutically active peptides, presenting both the advantages and challenges associated with this molecular class. The first part discusses current approaches to developing pharmaceutically active peptides, including case studies of the use of peptidic drugs in cancer and AIDS therapy. The second part surveys strategies for the development and targeting of peptidic drugs. With its integration of biochemical, pharmaceutical and clinical research, this work reveals the full picture of modern peptide drug research in a single volume, making it an invaluable reference for medicinal chemists, biochemists, biotechnologists, and those in the pharmaceutical and biotechnological industries.

Directory of Graduate Research

Directory of Graduate Research
A Book

by American Chemical Society. Committee on Professional Training

  • Publisher : Unknown Publisher
  • Release : 2005
  • Pages : 329
  • ISBN : 9876543210XXX
  • Language : En, Es, Fr & De
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Faculties, publications and doctoral theses in departments or divisions of chemistry, chemical engineering, biochemistry and pharmaceutical and/or medicinal chemistry at universities in the United States and Canada.

Medicinal Chemistry and Drug Discovery: Nervous system agents

Medicinal Chemistry and Drug Discovery: Nervous system agents
A Book

by Alfred Burger

  • Publisher : Unknown Publisher
  • Release : 2003
  • Pages : 329
  • ISBN : 9876543210XXX
  • Language : En, Es, Fr & De
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Heterocyclic Chemistry in Drug Discovery

Heterocyclic Chemistry in Drug Discovery
A Book

by Jie Jack Li

  • Publisher : John Wiley & Sons
  • Release : 2013-04-26
  • Pages : 720
  • ISBN : 1118354435
  • Language : En, Es, Fr & De
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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.