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

Tetrahedron

Integrated Biosciences Graduate Program, University of Minnesota, MN 55812, USA; Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, USA; Department of Pharmacy Practice and Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, USA.

Published: June 2016


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Article Abstract

Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for their -mycobacterial activity on 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 -mycobacterial activity. Some of the key compounds have been evaluated for their -tubercular activity on H37Rv using 7H9 and GAST media. 7-Bromo-6-aminobenzoboroxole has been identified as the lead candidate compound for further development.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5021310PMC
http://dx.doi.org/10.1016/j.tet.2016.03.038DOI Listing

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