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

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.