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Structural Activity Relationship and Importance of Benzothiazole Derivatives in Medicinal Chemistry: A Comprehensive Review
Mini-Reviews in Organic Chemistry ( IF 2.3 ) Pub Date : 2020-05-01 , DOI: 10.2174/1570193x16666190204111502
Mahesh Bhat 1 , Shiddappa Lagamappa Belagali 2
Affiliation  

Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activities, with less toxic effects and their derivatives showed enhanced activities, which has proven Benzothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, antiallergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes benzothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.



中文翻译:

结构活性关系和苯并噻唑衍生物在药物化学中的重要性:综述

苯并噻唑(1,3-苯并噻唑)是杂环化合物之一,它是一种具有多种生物活性的弱碱。噻唑环中独特的次甲基中心使苯并噻唑成为最重要的杂环化合物。它是许多天然和合成生物活性分子的共同整体结构。苯并噻唑衍生物表现出多种活性,毒性作用较小,其衍生物显示出增强的活性,这已证明苯并噻唑支架是药物化学中的重要部分之一。含有苯并噻唑环的化合物具有多种药理活性,例如抗病毒,抗微生物,抗过敏,抗糖尿病,抗肿瘤,抗炎,驱蚊和抗癌,这使得苯并噻唑在药物化学中成为快速发展的有趣化合物。这篇综述简要地解释了苯并噻唑支架的重要的合成方法,并解释了在各种化学领域中都有应用的流行的苯并噻唑分子。基于包含苯并噻唑部分的各种药理活性进行了审查,并根据结构变化合理化了活性。关于苯并噻唑衍生物的文献表明,在C-2碳原子和C-6上进行取代是产生多种生物活性的原因。苯并噻唑支架的常见合成方法,也解释了流行的苯并噻唑分子,它们在化学的各个领域都有应用。基于包含苯并噻唑部分的各种药理活性进行了审查,并根据结构变化合理化了活性。关于苯并噻唑衍生物的文献表明,在C-2碳原子和C-6上进行取代是产生多种生物活性的原因。苯并噻唑支架的常见合成方法,也解释了流行的苯并噻唑分子,它们在化学的各个领域都有应用。基于包含苯并噻唑部分的各种药理活性进行了审查,并根据结构变化合理化了活性。关于苯并噻唑衍生物的文献表明,在C-2碳原子和C-6上进行取代是产生多种生物活性的原因。

更新日期:2020-05-01
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