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2-芳基苯并噻唑作为药物研发中的优势骨架。

2-Arylbenzothiazole as a privileged scaffold in drug discovery.

作者信息

Weekes A A, Westwell A D

机构信息

Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, Wales, UK.

出版信息

Curr Med Chem. 2009;16(19):2430-40. doi: 10.2174/092986709788682137.

Abstract

Substituted 2-arylbenzothiazoles have emerged in recent years as an important pharmacophore in a number of diagnostic and therapeutic settings. Attractive features of drug candidates based on this benzothiazole scaffold include their synthetic accessibility, and synthetic approaches to 2-arylbenzothiazole-based compounds will be reviewed here. Examples of 2-arylbenzothiazoles endowed with diagnostic/therapeutic activity include the 2-(4-aminophenyl)benzothiazole series, which has a remarkable activity profile in both the potential non-invasive diagnosis of Alzheimer's disease and as antitumour agents.

摘要

近年来,取代的2-芳基苯并噻唑已成为许多诊断和治疗领域的重要药效基团。基于这种苯并噻唑骨架的候选药物的吸引人之处包括其合成的可及性,本文将综述基于2-芳基苯并噻唑的化合物的合成方法。具有诊断/治疗活性的2-芳基苯并噻唑的例子包括2-(4-氨基苯基)苯并噻唑系列,其在阿尔茨海默病的潜在非侵入性诊断和作为抗肿瘤药物方面都具有显著的活性特征。

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