Heterocyclic Drug Discovery - Böcker

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.

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.

Oxazole, Isoxazole, Benzoxazole Based Drug Discovery offers complete coverage of oxazole and related molecules, both from natural and synthetic origin, with a focus on the reaction mechanisms, and medicinal, pharmacokinetic and computational aspects. New and contemporary methods of synthesis are discussed, with a special focus on green, environment-friendly procedures. Discussion of stereochemical studies, particularly on natural molecules, are included. Computational chemistry has emerged as an integral tool for drug discovery, hence this book explains how the drug candidate is established as suitable for clinical trials with the help of molecular docking and virtual screening modeling.This book offers a broad range of recent developments and detailed coverage of synthesis and biological activities of the drugs, and is an ideal reference guide to researchers working in organic and medicinal chemistry.

Imidazole-Based Drug Discovery covers all categories of imidazole and its derivatives, synthesis, pharmacological applications and drug-based studies. Imidazole scaffolds act as a channel between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. This book provides detailed coverage of several greener synthetic protocols and pharmacological applications of imidazole derivatives that are useful to researchers working on designing more promising clinical lead compounds with this scaffold. It also includes information on past decades of research on the synthesis and biological applications of imidazole derivatives.

This is an ideal resource for researchers in organic chemistry both in academic and industrial settings, as well as postgraduates in chemistry and medicinal chemistry.