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Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents
Tetrahedron (2016)
  • Mohammad A. Alam
  • Kriti Arora
  • Shirisha Gurrapu
  • Sravan K. Jonnalagadda
  • Grady L. Nelson
  • Paul Kiprof
  • Subash Jonnalagadda, Rowan University
  • Venkatram R. Mereddy
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.
  • Benzoboroxoles,
  • Nitrobenzoboroxole,
  • Aminobenzoboroxole,
  • Bromoaminobenzoboroxole,
  • anti-Tuberculosis agents
Publication Date
June, 2016
Citation Information
Mohammad A. Alam, Kriti Arora, Shirisha Gurrapu, Sravan K. Jonnalagadda, et al.. "Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents" Tetrahedron Vol. 72 Iss. 26 (2016) p. 3795 - 3801 ISSN: 0040-4020
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