Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents

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• 作者：Mohammad A. Alam^a ; Kriti Arora^b ; Shirisha Gurrapu^c ; Sravan K. Jonnalagadda^c ; Grady L. Nelson^c ; Paul Kiprof^d ; Subash C. Jonnalagadda^a ; ^e ; ^{jonnalagadda@rowan.edu" class="auth_mail" title="E-mail the corresponding author} ; Venkatram R. Mereddy^c ; ^d ; ^f ; ^{vmereddy@d.umn.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Benzoboroxoles ; Nitrobenzoboroxole ; Aminobenzoboroxole ; Bromoaminobenzoboroxole ; anti-Tuberculosis agents
• 刊名：Tetrahedron
• 出版年：2016
• 出版时间：30 June 2016
• 年：2016
• 卷：72
• 期：26
• 页码：3795-3801
• 全文大小：433 K

文摘

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.