4.7 Article

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

Journal

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume 61, Issue 9, Pages -

Publisher

AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.01205-17

Keywords

antimicrobial; antitubercular; drug resistance

Funding

  1. Bill and Melinda Gates Foundation
  2. NIAID of National Institutes of Health [R01AI099188]

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

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