Download or read book Benzodiazepine Based Drug Discovery written by Farzad Zamani and published by Elsevier. This book was released on 2022-08-16 with total page 340 pages. Available in PDF, EPUB and Kindle. Book 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

Download or read book Privileged Structures in Drug Discovery written by Larry Yet and published by John Wiley & Sons. This book was released on 2018-03-27 with total page 560 pages. Available in PDF, EPUB and Kindle. Book 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 synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.

Download or read book Benzodiazepines written by National Institute on Drug Abuse. Division of Research and published by . This book was released on 1981 with total page 116 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Poisonous Plants and Phytochemicals in Drug Discovery written by Andrew G. Mtewa and published by John Wiley & Sons. This book was released on 2020-12-22 with total page 444 pages. Available in PDF, EPUB and Kindle. Book excerpt: Focusing on phytochemicals and their potential for drug discovery, this book offers a comprehensive resource on poisonous plants and their applications in chemistry and in pharmacology. Provides a comprehensive resource on phytotoxins, covering historical perspectives, modern applications, and their potential in drug discovery Covers the mechanisms, benefits, risks and management protocols of phytotoxins in a scientific laboratory and the usefulness in drug discovery Presents chapters in a carefully designed, clear order, making it an ideal resource for the academic researcher or the industry professional at any stage in their career

Download or read book Benzodiazepines written by and published by . This book was released on 1981 with total page 116 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Naturally Occurring Benzodiazepines Endozepines and their Receptors written by Robert B. Raffa and published by CRC Press. This book was released on 2021-08-13 with total page 216 pages. Available in PDF, EPUB and Kindle. Book excerpt: Understanding and addressing the current opioid crisis requires knowledge of endogenous opioids (endorphins and enkephalins), but there is now evidence for a benzodiazepine crisis. Are there endogenous benzodiazepine-like substances—and what do they do? How do they affect antianxiety drugs and their adverse effects? Do they explain enigmatic prolonged benzodiazepine withdrawal syndrome? This book raises important questions about the clinical consequences of ignoring the existence of or understanding the potential influence of endogenous benzodiazepines on the therapeutic effect of benzodiazepines, their adverse effects, and the problems of withdrawal from them and other benzodiazepine receptor agonists. FEATURES Discusses endogenous benzodiazepine-like substances—what do they do, and do they affect antianxiety drugs and their adverse effects? Presents information on enigmatic prolonged benzodiazepine withdrawal syndrome Describes the compounds acting at the BDZ binding sites, both exogenous (classical BDZ drugs and BDZ from food and plants) and endogenous (endozepines) Assesses the putative interactions in physiology, pathology, and pharmacology of the compounds acting at the BDZ binding sites Dr. Raffa is Adjunct Professor at the University of Arizona College of Pharmacy and Professor Emeritus at Temple University School of Pharmacy. He has co-authored or edited several books on pharmacology and thermodynamics, is a co-editor of two journals, is a past president of the Mid-Atlantic Pharmacology Society, and is the recipient of research and teaching awards. Dr. Amantea is Associate Professor of Pharmacology at the Department of Pharmacy, Health and Nutritional Sciences of the University of Calabria (Italy), where she is the leader of the Stroke Research Unit at the Section of Preclinical and Translational Pharmacology operating in the frame of the Italian Stroke Organization (ISO) Basic Science. She is a member of the Editorial Board and the Guest Editor of the 2016 Neuroscience section of Current Opinion in Pharmacology (Elsevier), and the founder and the editor of the CRC Press Frontiers in Neurotherapeutics series.

Download or read book Molecular Aspects of Anticancer Drug DNA Interactions written by Stephen Neidle and published by CRC Press. This book was released on 1994-05-03 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: This cutting-edge book surveys the current knowledge on the mode of action of the major classes of DNA-interactive antitumor agents, providing information that could be crucial for the discovery of new therapeutic substances. It is an important reference for molecular biologists, cancer researchers, biochemists, biophysicists, and pharmacologists.

Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Download or read book Progress in drug research 50 1998 written by Ernst Jucker and published by Springer Science & Business Media. This book was released on 1998 with total page 384 pages. Available in PDF, EPUB and Kindle. Book excerpt: Progress in Drug Research is a prestigious book series (founded in 1959) which provides extensive expert-written reviews on a wide spectrum of highly topical areas in current pharmaceutical and pharmalogical research. Each volume contains fully cross-referencing indexes which link the volumes together, forming a virtually encyclopaedic work. The series thus serves as an important, time-saving source of information for researchers concerned with drug research and all those who need to keep abreast of the many recent developments in the quest for new and better medicines. Volume 50 in the series includes: P.N. Kaul: Drug discovery: Past, present and future M. Rohmer: Isoprenoid biosynthesis via the mevalonate -- independent route, a novel target for antibacterial drugs G. Edwards and A.H. Weston: Endothelium, -derived hyperpolarizing factor -- a critical appraisal R.W. Rockhold: Glutamatic involvement in psychomotor stimulant action J.M. Colacino and K.A. Staschke: The identification and development of antiviral agents for the treatment of chronic hepatitis B virus infection T.D. Johnson: Polyamines and cerebral ischemia

Download or read book The Benzodiazepines written by J. Marks and published by Springer. This book was released on 2012-02-23 with total page 111 pages. Available in PDF, EPUB and Kindle. Book 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.

Download or read book Improving and Accelerating Therapeutic Development for Nervous System Disorders written by Institute of Medicine and published by National Academies Press. This book was released on 2014-02-06 with total page 107 pages. Available in PDF, EPUB and Kindle. Book 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.

Download or read book Synthesis of Essential Drugs written by Ruben Vardanyan and published by Elsevier. This book was released on 2006-03-10 with total page 634 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Download or read book The Benzodiazepines Crisis written by John Peppin and published by Oxford University Press, USA. This book was released on 2021 with total page 289 pages. Available in PDF, EPUB and Kindle. Book excerpt: Misused, abused, diverted, and counterfeited, benzodiazepines have serious potential for substance use disorder, and are among the leading causes of drug-related overdose deaths. Evidence indicates that prolonged use of benzodiazepines causes a wide range of adverse reactions, and withdrawal can be particularly challenging. Nevertheless, these negative aspects have yet to be thoroughly addressed within the medical community and remain virtually unknown to patients. This book offers an in-depth discussion of the downsides of this overused class of drugs and calls for their rational and dramatically reduced usage.

Download or read book Versed written by Rae Armantrout and published by Wesleyan University Press. This book was released on 2010-08-01 with total page 143 pages. Available in PDF, EPUB and Kindle. Book excerpt: Winner of the 2010 Pulitzer Prize for Poetry Winner of the Pulitzer Prize for Poetry (2010) Winner of the National Book Critics Circle Award (2009) Rae Armantrout has always organized her collections of poetry as though they were works in themselves. Versed brings two of these sequences together, offering readers an expanded view of the arc of her writing. The poems in the first section, Versed, play with vice and versa, the perversity of human consciousness. They flirt with error and delusion, skating on a thin ice that inevitably cracks: "Metaphor forms / a crust / beneath which / the crevasse of each experience." Dark Matter, the second section, alludes to more than the unseen substance thought to make up the majority of mass in the universe. The invisible and unknowable are confronted directly as Armantrout's experience with cancer marks these poems with a new austerity, shot through with her signature wit and stark unsentimental thinking. Together, the poems of Versed part us from our assumptions about reality, revealing the gaps and fissures in our emotional and linguistic constructs, showing us ourselves where we are most exposed. A reader's companion is available at http://versedreader.site.wesleyan.edu/

Download or read book Synthesis of Best Seller Drugs written by Ruben Vardanyan and published by Academic Press. This book was released on 2016-01-07 with total page 868 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Download or read book Anxiolytics written by Mike Briley and published by Springer Science & Business Media. This book was released on 2000-09-01 with total page 200 pages. Available in PDF, EPUB and Kindle. Book excerpt: For over thirty years the benzodiazepines monopolised not only the anxiolytic market but also clinical and animal research in anxiety. Indeed many animal tests developed since the 1960s have been optimised for the benzodiazepines and some programmes have even screened candidates as potential anxiolytics on their benzodiazepine-like side-effects rather than their anxiolytic activity. With the realisation of the drawbacks of the benzodiazepines, namely their potential for tolerance and dependency, there has been a renewed interest in alternative anxiolytics both from existing drugs such as the tricyclic and monoamine oxidase antidepressants and from newer agents such as buspirone. In addition anxiety is no longer considered to be a unique entity but rather an umbrella term for a series of specific anxiety disorders such as panic disorder without or with agoraphobia, generalised anxiety disorder (GAD), specific phobias, social phobias and post-traumatic stress disorder (PTSD). These new clinical categories have opened another dimension in the therapy of anxiety requiring the optimisation of treatments for different syndromes. This book is a critical review of today's anxiolytics and those that may become the anxiolytics of tomorrow. What is clear is that currently there are few clinically satisfactory alternatives to the benzodiazepines for the treatment of acute anxiety. For chronic anxiety, it is generally agreed that benzodi azepines are not the treatment of first choice. The tricyclic and monoamine oxidase antidepressants, the serotonin reuptake inhibitors and buspirone offer better solutions for chronic anxiety but they are still far from being ideal.

Download or read book The Combinatorial Index written by Barry A. Bunin and published by Elsevier. This book was released on 1998-04-15 with total page 341 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods Serves as a laboratory manual for bench chemists Includes a chapter on linkers to assist in choice of linking strategy Discusses strengths and limitations of the various methods Contains a structural index showing functional group transformations in solid-phase synthesis