A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosisIn Vitro

We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis. The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentra...

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Veröffentlicht in:Antimicrobial agents and chemotherapy 2017-08, Vol.61 (9)
Hauptverfasser: Patel, Nipul, O'Malley, Theresa, Zhang, Yong-Kang, Xia, Yi, Sunde, Bjorn, Flint, Lindsay, Korkegian, Aaron, Ioerger, Thomas R, Sacchettini, Jim, Alley, M. R. K, Parish, Tanya
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Sprache:eng
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Zusammenfassung:We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis. The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentration [IC50] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC50 > 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.
ISSN:0066-4804
1098-6596
DOI:10.1128/AAC.01205-17