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首页> 外文期刊>RSC Advances >Regio- and diastereoselective synthesis of spiropyrroloquinoxaline grafted indole heterocyclic hybrids and evaluation of their anti-Mycobacterium tuberculosis activity
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Regio- and diastereoselective synthesis of spiropyrroloquinoxaline grafted indole heterocyclic hybrids and evaluation of their anti-Mycobacterium tuberculosis activity

机译：螺吡咯过喹喔啉接枝吲哚杂交杂交体的重组和非对映选择性合成及其抗结核分枝杆菌活性的评价

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摘要

An efficient and eco compatible approach for the regio- and stereoselective synthesis of structurally diverse novel hybrid heterocycles comprising spiropyrrolidine, indenoquinoxaline and indole structural units in excellent yields, has been achieved through a one-pot multicomponent process involving 1,3-dipolar cycloaddition as a key step. The 1,3-dipolar component is the azomethine ylide generated in situ from indenoquinoxaline and L -tryptophan and reacts with various substituted β-nitrostyrenes affording the spiroheterocyclic hybrids. The ring system thus created possesses two C–C and three C–N bonds and four adjacent stereogenic carbons, one of which is quaternary and the reaction proceeded with full diastereomeric control. All the synthesized compounds were assayed for their in vitro activity against Mycobacterium tuberculosis H37Rv using MABA assay. Interestingly, the compound bearing a 2-fluoro substituent on the aryl ring displayed an equipotent activity (MIC 1.56 μg mL ~(?1) ) to ethambutol against Mycobacterium tuberculosis H37Rv.
机译：通过一种涉及1,3-偶极环加装饰的一盆多组分方法，实现了一种有效和ECO和立体选择性新型新型杂化杂交杂交杂交杂交杂交杂交杂交杂交杂交杂交杂交的兼容方法，涉及1,3-偶极环喷环加入的一盆多组分工艺关键步骤。 1,3-偶极组分是原位从茚上喹喔啉和L- -Tryptophan产生的氮杂甲酸盐ylide，并与提供螺旋螺旋状环杂交物的各种取代的β-硝化萘反应。如此产生的环系统具有两个C-C和三个C-N键，其中四个相邻的立体碳，其中一个是季铵，并且反应与全非对映异构对照进行。使用MABA测定法测定所有合成的化合物对分枝杆菌H37RV的体外活性。有趣的是，亚氟取代基在芳基上的化合物显示出抵抗分枝杆菌H37RV的乙胺醇的等态活性（MIC1.56μgml〜（α1））。

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