Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents.
Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents.
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DOI：
10.1016/j.tet.2016.03.038
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发表时间：
2016-06-30
期刊：
影响因子：
2.1
通讯作者：
Mereddy, Venkatram R.
中科院分区：
文献类型：
--
作者：
Alam, Mohammad A.;Arora, Kriti;Gurrapu, Shirisha;Jonnalagadda, Sravan K.;Nelson, Grady L.;Kiprof, Paul;Jonnalagadda, Subash C.;Mereddy, Venkatram R.
关键词：
以2-硼基苯甲醛为起始原料，合成了几种氨基苯并硼氧烷的衍生物。所有这些衍生物都被评估了它们对耻垢分枝杆菌的抗分枝杆菌活性和对乳腺癌细胞系MCF7的细胞毒性。基于这些研究，所有被测试的分子都被发现通常是无毒的，并且含有未取代(伯胺)的苯并硼氧杂环化合物被发现表现出良好的抗分枝杆菌活性。用7H9和GAST两种培养基对一些关键化合物进行了抗结核活性的评价。7-溴-6-氨基苯并氧杂4已被确定为进一步开发的主要候选化合物。
Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for their anti-mycobacterial activity on Mycobacterium smegmatis and cytotoxicity on breast cancer cell line MCF7. Based on these studies, all the tested molecules have been found to be generally non-toxic and benzoboroxoles with unsubstituted (primary) amines have been found to exhibit good anti-mycobacterial activity. Some of the key compounds have been evaluated for their anti-tubercular activity on Mycobacterium tuberculosis H37Rv using 7H9 and GAST media. 7-Bromo-6-aminobenzoboroxole 4 has been identified as the lead candidate compound for further development.
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