Benzodiazepine Based Drug Discovery Book

Benzodiazepine Based Drug Discovery


  • Author : Farzad Zamani
  • Publisher : Elsevier
  • Release Date : 2022-08-26
  • Genre: Science
  • Pages : 338
  • ISBN 10 : 9780323860109

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Benzodiazepine Based Drug Discovery Excerpt :

Benzodiazepine-Based Drug Discovery covers benzodiazepines and benzothiazepines, which constitute two pivotal classes of heterocyclic compounds widely used as core structures of medicinal drugs for the treatment of depression, epilepsy, seizures and muscle spasms. 1,4-Benzodiazepine, 1,5-benzodiazepine, and 1,5-benzothiazepine are the most studied groups of benzodiazepines and benzothiazepines because of their outstanding potential biological activities. This book offers a broad range of recent developments and detailed coverage of the synthesis and biological activities of the drugs based on benzodiazepine and benzothiazepine matrixes, and is an ideal reference guide to researchers working in organic and medicinal chemistry. The importance of these privileged pharmacophores is not limited to the treatment of psychotic disorders because minor changes in the structures can generate various biological activities. They represent a wide range of therapeutic functions such as anticonvulsant, antianxiety, anti-depressant, antiviral, anti-HIV, anti-inflammatory, anticoagulant, anti-obesity, endothelin antagonist, cholecystokinin antagonist, and vasopressin receptor antagonist activities. Presents detailed coverage of chemical structures and practical synthetic methods of benzodiazepines and benzothiazepines in drug discovery Compiles detailed in vivo and in vitro biological activity data of 1,4-benzodiazepine- and 1,5-benzodiazepine-based drugs that will help researchers design and develop innovative drugs Discusses promising avenues and potential challenges in the development of new benzodiazepines and benzothiazepines in medicinal drug synthesis

Privileged Structures in Drug Discovery Book

Privileged Structures in Drug Discovery


  • Author : Larry Yet
  • Publisher : John Wiley & Sons
  • Release Date : 2018-03-27
  • Genre: Medical
  • Pages : 560
  • ISBN 10 : 9781118145661

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Privileged Structures in Drug Discovery Excerpt :

A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic syn

Peripheral Benzodiazepine Receptors Book

Peripheral Benzodiazepine Receptors


  • Author : Eva Giesen-Crouse
  • Publisher : Academic Press
  • Release Date : 1993-05-05
  • Genre: Medical
  • Pages : 308
  • ISBN 10 : UOM:39015031796363

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Peripheral Benzodiazepine Receptors Excerpt :

Neuroscience Perspectives provides multidisciplinary reviews of topics in one of the most diverse and rapidly advancing fields in the life sciences. Whether you are a new recruit to neuroscience, or an established expert, look to this series for 'one-stop' sources of the historical, physiological, pharmacological, biochemical, molecular biological and therapeutic aspects of chosen research areas. Although peripheral type benzodiazepne recognition sites have been demonstrated in the brain and peripheral organs of various species for more than 10 years, the exact physiological function or pharmacological effects have not yet been established. Peripheral benzodiazepine literature is so overwhelming that the novice may find it virtually impossible to form a clear idea about the diverse findings. This volume, dedicated exclusively to pBR and their natural and synthetic ligands, puts the available data into perspective. A truly interdisciplinary approach has brought neuroscientists, cardiologists, endocrinologists, and immunologists together to work on the description of pBR-mediated effects. The chemistry, biochemistry, and molecular biology of the pBR receptor and its ligands are reviewed, their pharmacological usefulness is conjectured, and thus a true overview of the field is provided. * SPECIAL FEATURES * This volume follows the Neuroscience Perspectives brief of providing a historical background, pharmacological, biochemical and physiological aspects of research and therapeutic potential, of its chosen topic. * The peripheral benzodiazepine recognition site has been recognised for more than ten years, but the exact physiological and pharmacological effects have not yet been established.

The Benzodiazepines Book

The Benzodiazepines


  • Author : J. Marks
  • Publisher : Springer
  • Release Date : 2012-02-23
  • Genre: Medical
  • Pages : 111
  • ISBN 10 : 9401162050

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The Benzodiazepines Excerpt :

The story of the benzodiazepines is a fascinating one: the synthesis of a long series of inert compounds and the abandonment of the project: months later, the renewal of the project and the discovery that this compound R05-0690 (Librium ®) was a sedative and muscle relaxant in laboratory animals: the recognition that its postulated structure was wrong and that it was in fact a member of an entirely new chemical class: the excitement caused by the discovery of the powerful taming effect of the drug in wild animals: the even greater excitement in medical circles when its dramatic anxiety relieving effects were cstablished in humans: the subsequent enormous world wide usc of drugs of the benzodiazepine group. I have reason to know the story well for during that period I worked in various capacities in research, marketing and manage ment in the British subsidiary of F. Hoffmann-Ia Roche. It was during this period that I became interested in whether dependence on benzodiazepines could occur and if so to what extent, but felt that this could be examined best from outside the concern. Having now retired from Roche back to academic medicine I have taken the opportunity to examine and analyse the evidence.

Privileged Scaffolds in Medicinal Chemistry Book

Privileged Scaffolds in Medicinal Chemistry


  • Author : Stefan Bräse
  • Publisher : Royal Society of Chemistry
  • Release Date : 2015-11-20
  • Genre: Medical
  • Pages : 486
  • ISBN 10 : 9781782620303

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Privileged Scaffolds in Medicinal Chemistry Excerpt :

This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Good Chemistry Book

Good Chemistry


  • Author : Alex Baenninger
  • Publisher : McGraw Hill Professional
  • Release Date : 2004
  • Genre: Biography & Autobiography
  • Pages : 200
  • ISBN 10 : 0071426175

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Good Chemistry Excerpt :

The development of Valium by Roche Pharmaceutical and the entire benzodiazepine group of active substances was among the greatest accomplishments in 20th-century pharmacology. Good Chemistry combines a detailed account of this momentous development with an engaging biography of Leo Sternbach, the brilliant chemist who invented Valium and whose achievements heralded the beginning of a new era in research and therapeutics. This thought-provoking biographical history: Tells the fascinating life story of one of the 20th century's premier chemists Traces the developments that led to the invention of Valium Provides a cultural history of Valium and its impact on society

Pyrrolo Benzodiazepine Class of Privileged Medicinal Scaffolds Book

Pyrrolo Benzodiazepine Class of Privileged Medicinal Scaffolds


  • Author : Sumitra Nain
  • Publisher : LAP Lambert Academic Publishing
  • Release Date : 2011-08
  • Genre: Uncategoriezed
  • Pages : 76
  • ISBN 10 : 3845421517

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Pyrrolo Benzodiazepine Class of Privileged Medicinal Scaffolds Excerpt :

On account of the wide range of the biological properties displayed by benzodiazepine derived compounds, benzodiazepine scaffold have been considered among the most important privileged structures for drug discovery. The development of novel biological materials based on the privileged structure is an intense area of research. Global efforts are underway to develop chemotherapeutic agentsThe main thrust of work in the area of additional fused heterocyclic rings is stimulated by the isolation of a series of antitumor antibiotics such as anthramycin, sibiromycin, tomaymycin, prothacarin, chicamycins A, B and neothramycins A, B (to mention a few), from the pyrrolo[2,1-c][1,4]-benzodiazepine class of compounds These biosynthetically derived materials are well known for inhibiting DNA replication on account of the formation of DNA - antibiotic adduct .

Analogue based Drug Discovery Book

Analogue based Drug Discovery


  • Author : IUPAC
  • Publisher : John Wiley & Sons
  • Release Date : 2006-12-13
  • Genre: Science
  • Pages : 606
  • ISBN 10 : 9783527607495

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Analogue based Drug Discovery Excerpt :

The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds. Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them. The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability.

Receptor Binding in Drug Research Book

Receptor Binding in Drug Research


  • Author : Robert A. O'Brien
  • Publisher : CRC Press
  • Release Date : 2020-08-27
  • Genre: Science
  • Pages : 547
  • ISBN 10 : 9781000146776

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Receptor Binding in Drug Research Excerpt :

This book describes the applications of receptor techniques in many different areas in addition to conventional drug and neurotransmitter binding sites. It reviews humoral modulators such as a leukotrienes, interferon, platelet-derived growth factor, and novel endogenous ligands.

Frontiers in CNS Drug Discovery Book

Frontiers in CNS Drug Discovery


  • Author : Atta-ur Rahman
  • Publisher : Bentham Science Publishers
  • Release Date : 2011-08-12
  • Genre: Medical
  • Pages : 653
  • ISBN 10 : 9781608051595

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Frontiers in CNS Drug Discovery Excerpt :

"Frontiers in CNS Drug Discovery" is an Ebook series devoted to publishing the latest and the most important advances in Central Nervous System (CNS) drug design and discovery. Eminent scientists write contributions on all areas of rational drug design an

Sleep  Benzodiazepines and Performance Book

Sleep Benzodiazepines and Performance


  • Author : Ian Hindmarch
  • Publisher : Springer
  • Release Date : 2011-12-10
  • Genre: Medical
  • Pages : 228
  • ISBN 10 : 3642696619

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Sleep Benzodiazepines and Performance Excerpt :

The following papers were presented at an International Workshop on experi mental methodologies and research strategies in sleep, benzodiazepines and per formance during the VII. International Congress of Psychiatry in Vienna 1983. Authors were asked to examine and review the methods used and the results obtained from the various studies within their particular expertise and to provide guidelines for future strategies in the psychopharmacology of sleep. It has long been felt by sleep researchers, psychopharmacologists and clini cians that the effects of drugs on sleep or even sleep itself cannot be evaluated without reference to the daytime behaviour of the individual. Sleep and daytime performance are complementary aspects of the same circadian cycle. The modifi cation of sleep parameters by hypnotic medication must necessarily have an impact upon daytime behaviour. The overall change in a patient's daytime behaviour following nocturnal administration of a benzodiazepine is of importance when considering the toler ability and safety of the drug in clinical use. Alterations to the integrity of daytime performance also have consequences for that patient's subsequent sleep and nocturnal behaviour. Thus this workshop was conceived as a platform for examining the inter relationship of sleep, benzodiazepine hypnotics and daytime performance from pharmacological, psychological, experimental and clinical standpoints. The fol lowing papers also highlight the complexity of the interaction between sleep, patient, drug and daytime performance and emphasize the need to approach problem areas with appropriate research strategies and experimental method ologies.

Drug Discovery Handbook Book

Drug Discovery Handbook


  • Author : Shayne Cox Gad
  • Publisher : John Wiley & Sons
  • Release Date : 2005-06-24
  • Genre: Science
  • Pages : 1494
  • ISBN 10 : 9780471728771

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Drug Discovery Handbook Excerpt :

The Drug Discovery Handbook gives professionals a tool to facilitate drug discovery by bringing together, for the first time in one resource, a compendium of methods and techniques that need to be considered when developing new drugs. This comprehensive, practical guide presents an explanation of the latest techniques and methods in drug discovery, including: Genomics, proteomics, high-throughput screening, and systems biology Summaries of how these techniques and methods are used to discover new central nervous system agents, antiviral agents, respiratory drugs, oncology drugs, and more Specific approaches to drug discovery, including problems that are encountered, solutions to these problems, and limitations of various methods and techniques The thorough coverage and practical, scientifically valid problem-solving approach of Drug Discovery Handbook will serve as an invaluable aid in the complex task of developing new drugs.

Progress in Drug Research   Fortschritte der Arzneimittelforschung   Progr  s des Recherches Pharmaceutiques Book

Progress in Drug Research Fortschritte der Arzneimittelforschung Progr s des Recherches Pharmaceutiques


  • Author : Vijendra K. Singh
  • Publisher : Birkhäuser
  • Release Date : 2012-03-17
  • Genre: Medical
  • Pages : 388
  • ISBN 10 : 303487166X

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Progress in Drug Research Fortschritte der Arzneimittelforschung Progr s des Recherches Pharmaceutiques Excerpt :

Volume 45 of "Progress in Drug Research" contains eight reviews and the various indexes which facilitate its use and establish the connection with the previous volumes. The articles in this volume deal with neuro peptides as native immune modulators, with Calmodulin and with effects of cell stimuli and drugs on cellular activation, with recent advances in benzodiazepine receptor binding studies, with the medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor, with Serotonin uptake inhibitors, with computer-aided drug design, with natri uretic hormones and with the recent developments in the chemotherapy of osteoporosis. In the 36 years that PDR has existed, the Editor has enjoyed the valu able help and advice of many colleagues. Readers, the authors of the reviews and, last but not least, the reviewers have all contributed greatly to the success of this series. Although the comments received so far have generally been favorable, it is nevertheless necessary to analyze and to reassess the current position and the future direction of such a series of monographs. So far, it has been the Editor's intention to help disseminate information on the vast domain of drug research, and to provide the reader with a tool with which to keep abreast of the latest developments and trends. The reviews in PDR are useful to the nonspecialist, who can obtain an overview of a particular field of drug research in a relatively short time.

Improving and Accelerating Therapeutic Development for Nervous System Disorders Book

Improving and Accelerating Therapeutic Development for Nervous System Disorders


  • Author : Institute of Medicine
  • Publisher : National Academies Press
  • Release Date : 2014-02-06
  • Genre: Medical
  • Pages : 118
  • ISBN 10 : 9780309292498

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Improving and Accelerating Therapeutic Development for Nervous System Disorders Excerpt :

Improving and Accelerating Therapeutic Development for Nervous System Disorders is the summary of a workshop convened by the IOM Forum on Neuroscience and Nervous System Disorders to examine opportunities to accelerate early phases of drug development for nervous system drug discovery. Workshop participants discussed challenges in neuroscience research for enabling faster entry of potential treatments into first-in-human trials, explored how new and emerging tools and technologies may improve the efficiency of research, and considered mechanisms to facilitate a more effective and efficient development pipeline. There are several challenges to the current drug development pipeline for nervous system disorders. The fundamental etiology and pathophysiology of many nervous system disorders are unknown and the brain is inaccessible to study, making it difficult to develop accurate models. Patient heterogeneity is high, disease pathology can occur years to decades before becoming clinically apparent, and diagnostic and treatment biomarkers are lacking. In addition, the lack of validated targets, limitations related to the predictive validity of animal models - the extent to which the model predicts clinical efficacy - and regulatory barriers can also impede translation and drug development for nervous system disorders. Improving and Accelerating Therapeutic Development for Nervous System Disorders identifies avenues for moving directly from cellular models to human trials, minimizing the need for animal models to test efficacy, and discusses the potential benefits and risks of such an approach. This report is a timely discussion of opportunities to improve early drug development with a focus toward preclinical trials.

Privileged Structures in Drug Discovery Book

Privileged Structures in Drug Discovery


  • Author : Larry Yet
  • Publisher : John Wiley & Sons
  • Release Date : 2018-03-07
  • Genre: Medical
  • Pages : 560
  • ISBN 10 : 9781118686355

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Privileged Structures in Drug Discovery Excerpt :

A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic syn