2-Arylbenzothiazole as a privileged scaffold in drug discovery.

2-Arylbenzothiazole as a privileged scaffold in drug discovery.
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DOI:
10.2174/092986709788682137
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发表时间:
2009-06
影响因子:
4.1
通讯作者:
A. Weekes;A. Westwell
A. Weekes;A. Westwell
中科院分区:
医学3区
文献类型:
--
作者:
A. Weekes;A. Westwell

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近年来,取代的2-芳基苯并噻唑在许多诊断和治疗环境中作为重要的药效团出现。基于这种苯并噻唑骨架的候选药物的吸引力特征包括它们的合成可及性,以及2-芳基苯并噻唑基化合物的合成方法将在这里进行综述。具有诊断/治疗活性的2-芳基苯并噻唑的实例包括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剂两者中具有显著的活性特征。
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.