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

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 mole...

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Bibliographic Details
Published in:Tetrahedron 2016-06, Vol.72 (26), p.3795-3801
Main Authors: Alam, Mohammad A., Arora, Kriti, Gurrapu, Shirisha, Jonnalagadda, Sravan K., Nelson, Grady L., Kiprof, Paul, Jonnalagadda, Subash C., Mereddy, Venkatram R.
Format: Article
Language:English
Subjects:
Amines
Aminobenzoboroxole
anti-Tuberculosis agents
Benzoboroxoles
Biotechnology
Breast
Bromoaminobenzoboroxole
Cancer
Derivatives
Mycobacterium smegmatis
Mycobacterium tuberculosis
Nitrobenzoboroxole
Synthesis
Tetrahedrons
Tuberculosis
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Summary: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. [Display omitted]
ISSN:0040-4020
1464-5416
DOI:10.1016/j.tet.2016.03.038