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A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro.

ABSTRACT: We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis The compound had an MIC of 2 ?M in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 ?M and was active against intracellular bacteria (50% inhibitory concentration [IC₅₀] = 3.6 ?M) without cytotoxicity against eukaryotic cells (IC₅₀ > 100 ?M). We isolated resistant mutants (MIC ? 100 ?M), which had mutations in Rv1683, Rv3068c, and Rv0047c.

SUBMITTER: Patel N

PROVIDER: S-EPMC5571309 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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A Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro.

Patel Nipul N O'Malley Theresa T Zhang Yong-Kang YK Xia Yi Y Sunde Bjorn B Flint Lindsay L Korkegian Aaron A Ioerger Thomas R TR Sacchettini Jim J Alley M R K MRK Parish Tanya T

Antimicrobial agents and chemotherapy 20170824 9

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, a ...[more]

PMID: 28674058

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