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首页> 外文期刊>RSC Advances >Synthesis of novel dispiropyrrolothiazoles by three-component 1,3-dipolar cycloaddition and evaluation of their antimycobacterial activity
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Synthesis of novel dispiropyrrolothiazoles by three-component 1,3-dipolar cycloaddition and evaluation of their antimycobacterial activity

机译：三组分1，3-偶极环加成反应合成新型双螺并吡咯并噻唑及其抗分枝杆菌活性

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摘要

In an on-going effort to develop novel anti-tubercular agents, a series of original dispiropyrrolothiazole derivatives have been synthesized by three-component 1,3-dipolar cycloaddition of (E)-3-arylidene-1phenyl- pyrrolidine-2,5-diones, 1,3-thiazolane-4-carboxylic acid and cyclic diketones. The stereochemistry of the spiranic adducts has been confirmed by an X-ray diffraction analysis. Theoretical calculations have been carried out using DFT approach at the B3LYP/6-31G(d, p) level allowing an explanation for the observed regio-and stereoselectivity. The newly synthesized compounds were screened in vitro against Mycobacterium tuberculosis H37Rv and the most active compounds were tested for cytotoxicity studies. Some compounds exhibited significant activity, in particular dispiropyrrolothiazole derivatives 15c and 15f emerged as the most promising antitubercular agents.
机译：在开发新型抗结核药的持续努力中，通过（E）-3-芳基-1苯基-吡咯烷-2,5-的三组分1,3-偶极环加成反应，合成了一系列原始的双螺并吡咯并噻唑衍生物。二酮，1，3-噻唑烷-4-羧酸和环状二酮。螺状加合物的立体化学已通过X射线衍射分析证实。使用DFT方法在B3LYP / 6-31G（d，p）水平进行了理论计算，从而可以解释所观察到的区域选择性和立体选择性。在体外针对结核分枝杆菌H37Rv筛选了新合成的化合物，并测试了最具活性的化合物进行细胞毒性研究。一些化合物表现出显着的活性，特别是双螺并吡咯并噻唑衍生物15c和15f作为最有希望的抗结核药出现。

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