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.
Bibliographical noteFunding Information:
The work was funded, in part by the Intramural Research Program at NIAID, National Institutes of Health . We thank Dr. Clifton E. Barry and Dr. Helena Boshoff (NIAID, NIH) for their guidance with the study. We thank Dr. John Dahl, Department of Biology, University of Minnesota Duluth for kindly providing Mycobacterium smegmatis culture. We thank the Departments of Chemistry and Biochemistry at Rowan University and University of Minnesota Duluth as well as the Integrated Biosciences Program.
- anti-Tuberculosis agents