Abstract

A series of benzothiazole and benzoxazole linked 1,4-disubstituted 1,2,3-triazoles was synthesized through copper(I) catalyzed azide-alkyne cycloaddition reaction. FTIR, ¹H, ¹³C-NMR and HRMS techniques were used to examine the structure of synthesized derivatives. Further, these triazole derivatives were screened for in vitro antibacterial activities against two Gram-positive bacteria S. aureus, B. subtilis; two Gram-negative bacteria E. coli and K. pneumoniae by serial dilution technique, reflecting moderate to good activity. Compound 7s exhibited promising antibacterial activity among all the synthesized triazoles.

Graphic abstract

中文翻译：

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苯并噻唑和苯并恶唑取代的1,2,3-三唑的合成及抑菌活性

摘要

通过铜（I）催化的叠氮化物-炔烃环加成反应，合成了一系列苯并噻唑和苯并恶唑连接的1,4-二取代的1,2,3-三唑。FTIR，¹ H，¹³ C-NMR和HRMS技术用于检查合成衍生物的结构。此外，筛选了这些三唑衍生物对两种革兰氏阳性细菌金黄色葡萄球菌，枯草芽孢杆菌（B.subtilis）的体外抗菌活性。通过连续稀释技术将两种革兰氏阴性细菌大肠杆菌和肺炎克雷伯氏菌反映出中等至良好的活性。在所有合成的三唑中，化合物7s显示出有希望的抗菌活性。

图形摘要