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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

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,Raimund Mannhold,Hugo Kubinyi,Gerd Folkers
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.

Carbohydrate based Drug Discovery

Carbohydrate based Drug Discovery Book
Author : Chi-Huey Wong
Publisher : John Wiley & Sons
Release : 2006-03-06
ISBN : 3527605789
Language : En, Es, Fr & De

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Book Description :

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: > Chemical Synthesis of Carbohydrates > Carbohydrate Biosynthesis and Metabolism > Carbohydrate Analysis > Cellular Functions of Carbohydrates > Development of Carbohydrate-based Drugs A premier resource for carbohydrate chemists and drug developers, this comprehensive two-volume work contains contributions by more than 50 of the world's leading carbohydrate chemists.

Kinase Drug Discovery

Kinase Drug Discovery Book
Author : Richard A. Ward,Frederick W. Goldberg
Publisher : Royal Society of Chemistry
Release : 2018-10-10
ISBN : 1788010833
Language : En, Es, Fr & De

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Book Description :

Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years.

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.

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.

Green Sustainable Process for Chemical and Environmental Engineering and Science

Green Sustainable Process for Chemical and Environmental Engineering and Science Book
Author : Dr. Inamuddin,Rajender Boddula,Mohd Imran Ahamed,Abdullah M. Asiri
Publisher : Elsevier
Release : 2020-12-01
ISBN : 0128218991
Language : En, Es, Fr & De

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Book Description :

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

Drug Discovery for Psychiatric Disorders

Drug Discovery for Psychiatric Disorders Book
Author : Zoran Rankovic,Richard Hargreaves,Matilda Bingham
Publisher : Royal Society of Chemistry
Release : 2012-10-08
ISBN : 1849734941
Language : En, Es, Fr & De

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Book Description :

The discovery and development of effective medicines for the treatment of psychiatric disorders such as schizophrenia and depression has been heralded as one of the great medical achievements of the past century. Indeed, the profound impact of these medicines on our understanding of the pathophysiology underlying these diseases, the treatment of psychiatric patients and even our social perception of mental illnesses cannot be underestimated. However, there is still an urgent medical need for even more effective, safe and well-tolerated treatments. For example, currently available treatments for schizophrenia address mainly the positive symptoms and largely neglect the negative symptoms and cognitive disfunction which greatly impact overall morbidity. Similarly, whilst the current first line antidepressants show significantly improved side effect profiles compared to the first generation therapies, there still up to 40% of patients who are treatment resistant, and even in the patient population which responds well, the onset of action is slow at typically 2-3 weeks. The aim of this book is to provide the first point of call for those involved or just interested in this rapidly expanding and increasingly fragmented field of research and drug discovery. The editors will combine their wide ranging experience and extensive network of contacts with leading scientists and opinion leaders in this field to provide an authoritative reference text covering the evolution, major advances, challenges and future directions in drug discovery and medicinal chemistry for major psychiatric disorders, such as schizophrenia, depression, anxiety, ADHD, bipolar disorder, addiction and autism.

Methods and Algorithms for Molecular Docking Based Drug Design and Discovery

Methods and Algorithms for Molecular Docking Based Drug Design and Discovery Book
Author : Dastmalchi, Siavoush
Publisher : IGI Global
Release : 2016-05-03
ISBN : 1522501169
Language : En, Es, Fr & De

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Book Description :

The role of technology in the medical field has resulted in significant developments within the pharmaceutical industry. Computational approaches have emerged as a crucial method in further advancing drug design and development. Methods and Algorithms for Molecular Docking-Based Drug Design and Discovery presents emerging research on the application of computer-assisted design methods for drugs, emphasizing the benefits and improvements that molecular docking has caused within the pharmaceutical industry. Focusing on validation methods, search algorithms, and scoring functions, this book is a pivotal resource for professionals, researchers, students, and practitioners in the field of theoretical and computational chemistry.

Scaffold Hopping in Medicinal Chemistry

Scaffold Hopping in Medicinal Chemistry Book
Author : Nathan Brown
Publisher : John Wiley & Sons
Release : 2013-11-06
ISBN : 3527665161
Language : En, Es, Fr & De

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Book Description :

This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here.

Anti fibrotic Drug Discovery

Anti fibrotic Drug Discovery Book
Author : Jehrod Brenneman,Malliga R. Iyer
Publisher : Royal Society of Chemistry
Release : 2020-02-28
ISBN : 178801510X
Language : En, Es, Fr & De

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Book Description :

Fibrosis is a condition with globally high unmet medical need, and as such is a highly active area of academic and pharmaceutical research covering multiple treatment targets, organs, tissues and therapeutic approaches. Anti-fibrotic Drug Discovery is a single source reference for the latest drug-discovery approaches to tackle fibrosis in various tissues, comprehensively covering recent success and future perspectives on emerging therapeutic intervention points. The book highlights significant pre-clinical and clinical drugs currently being developed globally for this disorder. This book is ideal for postgraduate students and researchers with an interest in anti-fibrotic drug discovery as well as clinicians specialising in liver, kidney, heart and lung disease, in which fibrosis plays a key role in pathology.

Chemokines

Chemokines Book
Author : Nuska Tschammer
Publisher : Springer
Release : 2015-03-02
ISBN : 3319140604
Language : En, Es, Fr & De

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Book Description :

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.

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.

Drug Discovery Approaches for the Treatment of Neurodegenerative Disorders

Drug Discovery Approaches for the Treatment of Neurodegenerative Disorders Book
Author : Adeboye Adejare
Publisher : Academic Press
Release : 2016-09-20
ISBN : 0128028114
Language : En, Es, Fr & De

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Book Description :

Drug Discovery Approaches for the Treatment of Neurodegenerative Disorders: Alzheimer’s Disease examines the drug discovery process for neurodegenerative diseases by focusing specifically on Alzheimer’s Disease and illustrating the paradigm necessary to ensure future research and treatment success. The book explores diagnosis, epidemiology, drug discovery strategies, current therapeutics, and much more to provide a holistic approach to the discovery, development, and treatment of Alzheimer’s Disease. Through its coverage of the latest research in targeted drug design, preclinical studies, and mouse and rat models, the book is a must-have resource for all pharmaceutical scientists, pharmacologists, neuroscientists, and clinical researchers working in this area. It illustrates why these drugs tend to fail at the clinical stage, and examines Alzheimer’s Disease within the overall context of improving the drug discovery process for the treatment of other neurodegenerative disorders. Provides a compilation of chemical considerations required in drug discovery for the treatment of neurodegenerative disorders Examines different classes of compounds currently being used in discovery and development stages Explores in vitro and in vivo models with respect to their ability to translate these models to human conditions Distills the most significant information across multiple areas of Alzheimer’s disease research to provide a single, comprehensive, and balanced resource

Frontiers in Clinical Drug Research Alzheimer Disorders Volume 7

Frontiers in Clinical Drug Research   Alzheimer Disorders  Volume 7 Book
Author : Atta-ur-Rahman
Publisher : Bentham Science Publishers
Release : 2018-11-02
ISBN : 1681085607
Language : En, Es, Fr & De

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Book Description :

Frontiers in Clinical Drug Research - Alzheimer Disorders is a book series concerned with Alzheimer's disease (AD), a disease that causes dementia, or loss of brain function. This disease affects parts of the brain that affect memory, thought, and language. Chapters in each volume focus on drug research with special emphasis on clinical trials, research on drugs in advanced stages of development and cure for Alzheimer’s disease and related disorders.

Analogue based Drug Discovery II

Analogue based Drug Discovery II Book
Author : János Fischer,C. Robin Ganellin
Publisher : John Wiley & Sons
Release : 2010-08-24
ISBN : 9783527632121
Language : En, Es, Fr & De

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Book Description :

Born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together constitute the first systematic approach to drug analog development. Of interest to virtually every researcher working in drug discovery and pharmaceutical chemistry.

Drug Discovery and Evaluation Pharmacological Assays

Drug Discovery and Evaluation  Pharmacological Assays Book
Author : Hans Vogel
Publisher : Springer Science & Business Media
Release : 2007-10-30
ISBN : 3540714200
Language : En, Es, Fr & De

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Book Description :

The new edition of this successful reference offers both cutting-edge and classic pharmacological methods. Thoroughly revised and expanded to two volumes, it offers an updated selection of the most frequently used assays for reliably detecting the pharmacological effects of potential drugs. Every chapter has been updated, and numerous assays have been added. Each of the more than 1,000 assays comprises a detailed protocol outlining purpose and rationale, and a critical assessment of the results and their pharmacological and clinical relevance.

Directory of Graduate Research

Directory of Graduate Research Book
Author : American Chemical Society. Committee on Professional Training
Publisher : Unknown
Release : 2005
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

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.