title: Synthesis and evaluation of functionalized benzoboroxoles as potentialanti-tuberculosis agents.
abstract: Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for theiranti-mycobacterial activity onMycobacterium smegmatisand 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 goodanti-mycobacterial activity. Some of the key compounds have been evaluated for theiranti-tubercular activity onMycobacterium tuberculosisH37Rv using 7H9 and GAST media. 7-Bromo-6-aminobenzoboroxole4has been identified as the lead candidate compound for further development.
authors.affiliation: Department of Chemistry and Biochemistry, Rowan University, Glassboro, NJ 08028, USA.
authors.forename: Mohammad A
authors.initials: MA
authors.lastname: Alam
authors.affiliation: Tuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Disease, National Institutes of Health, Bethesda, Maryland 20892, USA.
authors.forename: Kriti
authors.initials: K
authors.lastname: Arora
authors.affiliation: Integrated Biosciences Graduate Program, University of Minnesota, MN 55812, USA.
authors.forename: Shirisha
authors.initials: S
authors.lastname: Gurrapu
authors.affiliation: Integrated Biosciences Graduate Program, University of Minnesota, MN 55812, USA.
authors.forename: Sravan K
authors.initials: SK
authors.lastname: Jonnalagadda
authors.affiliation: Integrated Biosciences Graduate Program, University of Minnesota, MN 55812, USA.
authors.forename: Grady L
authors.initials: GL
authors.lastname: Nelson
authors.affiliation: Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, USA.
authors.forename: Paul
authors.initials: P
authors.lastname: Kiprof
authors.affiliation: Department of Chemistry and Biochemistry, Rowan University, Glassboro, NJ 08028, USA; Department of Biomedical and Translational Sciences, Rowan University, Glassboro, NJ 08028, USA.
authors.forename: Subash C
authors.initials: SC
authors.lastname: Jonnalagadda
authors.affiliation: 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.
authors.forename: Venkatram R
authors.initials: VR
authors.lastname: Mereddy
keywords: Benzoxaboroles; aminobenzoxaborole; anti-tuberculosis agents; bromoaminobenzoxaborole; nitrobenzoxaborole