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Piperidine Based Drug Discovery

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Piperidine Based Drug Discovery

Piperidine Based Drug Discovery Book
Author : Ruben Vardanyan
Publisher : Heterocyclic Drug Discovery
Release : 2017-06-14
ISBN : 9780128051573
Language : En, Es, Fr & De

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Book Description :

10.22 Piperidine-Based Gastric Antisecretory Drugs -- 10.23 Piperidine-Based Hypoglycemic Drugs -- 10.24 Piperidine-Based Drugs Used in the Treatment of Rheumatoid Arthritis -- 10.25 Piperidine-Based Nicotinic Cholinomimetics -- 10.26 Piperidine-Based Immunosuppresant Drugs -- 10.27 Conclusion -- Index-Trade Names -- Index-Substance Classes -- Back Cover

Piperidine Based Drug Discovery

Piperidine Based Drug Discovery Book
Author : Ruben Vardanyan
Publisher : Elsevier
Release : 2017-06-12
ISBN : 0128134283
Language : En, Es, Fr & De

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Book Description :

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

Drug Discovery with Privileged Building Blocks

Drug Discovery with Privileged Building Blocks Book
Author : Jie Jack Li,Minmin Yang
Publisher : CRC Press
Release : 2021-10-21
ISBN : 1000416011
Language : En, Es, Fr & De

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Book Description :

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.

Small Molecule Scaffold Synthesis One bead One compound Library Synthesis and Method Development in Drug Discovery

Small Molecule Scaffold Synthesis  One bead One compound Library Synthesis  and Method Development in Drug Discovery Book
Author : Seth M. Dixon
Publisher : Unknown
Release : 2006
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Download Small Molecule Scaffold Synthesis One bead One compound Library Synthesis and Method Development in Drug Discovery book written by Seth M. Dixon, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Synthetic Methods in Drug Discovery

Synthetic Methods in Drug Discovery Book
Author : David C Blakemore,Paul M Doyle,Yvette M Fobian
Publisher : Royal Society of Chemistry
Release : 2016-07-15
ISBN : 178262791X
Language : En, Es, Fr & De

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Book Description :

Building on key reactions presented in Volume 1, Synthetic Methods in Drug Discovery Volume 2 covers a range of important reaction types including organometallic chemistry, fluorination approaches and asymmetric methods as well as new and exciting areas such as Csp2-Csp3 couplings, catalytic amide bond forming reactions, hydrogen borrowing chemistry and methods to access novel motifs and monomers. This book provides both academic and industrial perspectives on 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. Moreover, key opportunities in expanding chemical space are presented, including the increasingly important syntheses that introduce three-dimensional molecular shape. 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.

Privileged Structures in Drug Discovery

Privileged Structures in Drug Discovery Book
Author : Larry Yet
Publisher : John Wiley & Sons
Release : 2018-03-07
ISBN : 1118686357
Language : En, Es, Fr & De

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Book Description :

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.

Synthesis of Essential Drugs

Synthesis of Essential Drugs Book
Author : Ruben Vardanyan,Victor Hruby
Publisher : Elsevier
Release : 2006-03-10
ISBN : 9780080462127
Language : En, Es, Fr & De

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Book Description :

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

Privileged Structures in Drug Discovery

Privileged Structures in Drug Discovery Book
Author : Larry Yet
Publisher : John Wiley & Sons
Release : 2018-03-27
ISBN : 1118145666
Language : En, Es, Fr & De

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Book Description :

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.

Fragment based Drug Discovery

Fragment based Drug Discovery Book
Author : Daniel A. Erlanson,Wolfgang Jahnke
Publisher : John Wiley & Sons
Release : 2016-02-23
ISBN : 352733775X
Language : En, Es, Fr & De

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Book Description :

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.

Fragment Based Drug Discovery

Fragment Based Drug Discovery Book
Author : Steven Howard,Chris Abell
Publisher : Royal Society of Chemistry
Release : 2015-07-03
ISBN : 1849739080
Language : En, Es, Fr & De

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Book Description :

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.

Tailored Functional Materials

Tailored Functional Materials Book
Author : Kalisadhan Mukherjee,Rama Kanta Layek,Debasis De
Publisher : Springer Nature
Release : 2022-10-17
ISBN : 9811925720
Language : En, Es, Fr & De

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Book Description :

This book presents the select proceedings of the International Symposium entitled “Materials of the Millennium: Emerging Trends and Future Prospects” (MMETFP 2021). It discusses the synthesis, tailoring, and characterization of different materials for functional applications in various sectors which include but not limited to energy, environment, biomedical/ health care, construction, transportation etc. Topics covered in this book are synthesis and characterization of polymers, ceramics, composites, biomaterials, carbon-based nanostructures as well as materials for green environment, structural materials, modeling and simulation of materials. The book also covers the topic of emerging trends in nanostructured materials, thin films, and devices. The book is useful for students, researchers, and professionals working in the various areas of materials science and engineering.

Peptidomimetics in Organic and Medicinal Chemistry

Peptidomimetics in Organic and Medicinal Chemistry Book
Author : Antonio Guarna,Andrea Trabocchi
Publisher : John Wiley & Sons
Release : 2014-03-14
ISBN : 1118683145
Language : En, Es, Fr & De

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Book Description :

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.

Peptide based Drug Discovery

Peptide based Drug Discovery Book
Author : Ved Srivastava
Publisher : Royal Society of Chemistry
Release : 2017-06-22
ISBN : 1788011716
Language : En, Es, Fr & De

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Book Description :

With potentially high specificity and low toxicity, biologicals offer promising alternatives to small-molecule drugs. Peptide therapeutics have again become the focus of innovative drug development efforts backed up by a resurgence of venture funds and small biotechnology companies. What does it take to develop a peptide-based medicine? What are the key challenges and how are they overcome? What are emerging therapeutics for peptide modalities? This book answers these questions with a holistic story from molecules to medicine, combining the themes of design, synthesis and clinical applications of peptide-based therapeutics and biomarkers. Chapters are written and edited by leaders in the field from industry and academia and they cover the pharmacokinetics of peptide therapeutics, attributes necessary for commercially successful metabolic peptides, medicinal chemistry strategies for the design of peptidase-resistant peptide analogues, disease classes for which peptide therapeutic are most relevant, and regulatory issues and guidelines. The critical themes covered provide essential background information on what it takes to develop peptide-based medicine from a chemistry perspective and views on the future of peptide drugs. This book will be a valuable resource not only as a reference book for the researcher engaged in academic and pharmaceutical setting, from basic research to manufacturing and from organic chemistry to biotechnology, but also a valuable resource to graduate students to understand discovery and development process for peptide-based medicine.

High Throughput Lead Optimization in Drug Discovery

High Throughput Lead Optimization in Drug Discovery Book
Author : Tushar Kshirsagar
Publisher : CRC Press
Release : 2008-03-04
ISBN : 1420006967
Language : En, Es, Fr & De

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Book Description :

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

Computational and Structural Approaches to Drug Discovery

Computational and Structural Approaches to Drug Discovery Book
Author : Robert Stroud,Janet Finer-Moore
Publisher : Royal Society of Chemistry
Release : 2007-10-31
ISBN : 1847557961
Language : En, Es, Fr & De

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Book Description :

Computational methods impact all aspects of modern drug discovery and most notably these methods move rapidly from academic exercises to becoming drugs in clinical trials... This insightful book represents the experience and understanding of the global experts in the field and spotlights both the structural and medicinal chemistry aspects of drug design. The need to 'encode' the factors that determine adsorption, distribution, metabolism, excretion and toxicology are explored, as they remain the critical issues in this area of research. This indispensable resource provides the reader with: * A rich understanding of modern approaches to docking * A comparison and critical evaluation of state-of-the-art methods * Details on harnessing computational methods for both analysis and prediction * An insight into prediction potencies and protocols for unbiased evaluations of docking and scoring algorithms * Critical reviews of current fragment based methods with perceptive applications to kinases Addressing a wide range of uses of protein structures for drug discovery the Editors have created and essential reference for professionals in the pharmaceutical industry and moreover an indispensable core text for all graduate level courses covering molecular interactions and drug discovery.

Structure based Design of Drugs and Other Bioactive Molecules

Structure based Design of Drugs and Other Bioactive Molecules Book
Author : Arun K. Ghosh,Sandra Gemma
Publisher : John Wiley & Sons
Release : 2014-08-11
ISBN : 3527333657
Language : En, Es, Fr & De

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Book Description :

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.

Green Approaches in Medicinal Chemistry for Sustainable Drug Design

Green Approaches in Medicinal Chemistry for Sustainable Drug Design Book
Author : Bimal K. Banik
Publisher : Elsevier
Release : 2020-04-09
ISBN : 0128175923
Language : En, Es, Fr & De

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Book Description :

Extensive experimentation and high failure rates are a well-recognised downside to the drug discovery process, with the resultant high levels of inefficiency and waste producing a negative environmental impact. Sustainable and Green Approaches in Medicinal Chemistry reveals how medicinal and green chemistry can work together to directly address this issue. After providing essential context to the growth of green chemistry in relation to drug discovery in Part 1, the book goes on to identify a broad range of practical methods and synthesis techniques in Part 2. Part 3 reveals how medicinal chemistry techniques can be used to improve efficiency, mitigate failure and increase the environmental benignity of the entire drug discovery process, whilst Parts 4 and 5 discuss natural products and microwave-induced chemistry. Finally, the role of computers in drug discovery is explored in Part 6. Identifies novel and cost effective green medicinal chemistry approaches for improved efficiency and sustainability Reflects on techniques for a broad range of compounds and materials Highlights sustainable and green chemistry pathways for molecular synthesis

Structure Based Drug Design

Structure Based Drug Design Book
Author : Pandi Veerapandian
Publisher : Routledge
Release : 2018-03-29
ISBN : 1351413066
Language : En, Es, Fr & De

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Book Description :

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!

Bioactive Peptides in Drug Discovery and Design

Bioactive Peptides in Drug Discovery and Design Book
Author : John Matsoukas,Thomas Mavromoustakos
Publisher : IOS Press
Release : 1999
ISBN : 9789051994254
Language : En, Es, Fr & De

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Book Description :

As in previous editions, the focus in ESSENTIAL MATHEMATICS with APPLICATIONS remains on the Aufmann Interactive Method (AIM). Students are encouraged to be active participants in the classroom and in their own studies as they work through the How To examples and the paired Examples and You Try It problems. Student engagement is crucial to success. Presenting students with worked examples, and then providing them with the opportunity to immediately solve similar problems, helps them build their confidence and eventually master the concepts. Simplicity is key in the organization of this edition, as in all other editions. All lessons, exercise sets, tests, and supplements are organized around a carefully constructed hierarchy of objectives. Each exercise mirrors a preceding objective, which helps to reinforce key concepts and promote skill building. This clear, objective-based approach allows students to organize their thoughts around the content, and supports instructors as they work to design syllabi, lesson plans, and other administrative documents. New features like Focus on Success, Apply the Concept, and Concept Check add an increased emphasis on study skills and conceptual understanding to strengthen the foundation of student success. The Ninth Edition also features a new design, enhancing the Aufmann Interactive Method and making the pages easier for both students and instructors to follow. Available with InfoTrac Student Collections http://gocengage.com/infotrac.

Anti Inflammatory Drug Discovery

Anti Inflammatory Drug Discovery Book
Author : Jeremy I. Levin,Stefan Laufer
Publisher : Royal Society of Chemistry
Release : 2012-07-18
ISBN : 1849735344
Language : En, Es, Fr & De

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Book Description :

Anti-Inflammatory Drug Discovery provides a comprehensive review of recent medicinal chemistry approaches to a variety of important therapeutic targets and provides a key reference for those interested in the prosecution of modern drug discovery programs directed at anti-inflammatory mechanisms of action. The editors, with extensive experience in this field, have selected key thought-leaders who will bring their experience to the medicinal chemistry literature for each target, ranging from components of the arachadonic acid cascade, to kinases, GPCRs, sphingolipids and others, to summarize its background biology and detail new insights, major advances and issues related to bringing new anti-inflammatory therapies to market. Consisting of five main sections key targets covered will include the AA Cascade: mPGES1, cPLA2, Leukotriene A4 Hydrolase, CRTH2; Kinases: P38/PDE4, MAPKAP Kinase 2 (MK2), Syk Kinase Inhibitors, Jak Kinases, IKK , Bruton's Tyrosine Kinase; GPCRs: CCR1, CCR2 Antagonists, CB2 Agonists; Sphingolipids: S1P1 Receptor Agonists, Sphingosine Lyase and Sphingosine Kinase 1 and a final miscellaneous section that looks at Non-Steroidal Dissociated Glucocorticoid Receptor Agonists. The book will be essential reading for pharmacologists, medicinal chemists and pharmaceutical scientists working in industry and academia.