Benzodiazepine Based Drug Discovery

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

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.

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

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

"Benzodiazepines were developed to treat legitimate medical needs. However, unbridled success and prescribing beyond their intended duration of use and the available data has led to excessive prescribing, extended utilization beyond good therapeutic practice, and unintended adverse effects and substance use disorder. This book is the first to bring to light and discuss the largely unrecognized and enigmatic problem of an exceedingly prolonged withdrawal syndrome from benzodiazepines that can persist for months or years in susceptible patients, and the medical need for better evidence-based prescribing of benzodiazepines, and a call for the recognition and better treatment of the prolonged withdrawal syndrome"--

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.

Provides an expanded view of the arc of the author's writing, collecting poems dealing with the perversity of human consciousness and the confrontation of the invisible experienced during the author's bout with cancer.

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