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

We identified a novel 6-benzyl ether benzoxaborole with potent activity against 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 [IC ] = 3.6 μM) without...

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Bibliographic Details
Published in:Antimicrobial agents and chemotherapy 2017-09, Vol.61 (9)
Main Authors: 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
Format: Article
Language:English
Subjects:
Antitubercular Agents - adverse effects
Antitubercular Agents - pharmacology
Cell Line, Tumor
Drug Resistance, Bacterial - genetics
Hep G2 Cells
Humans
Mechanisms of Resistance
Microbial Sensitivity Tests
Mycobacterium tuberculosis - drug effects
Mycobacterium tuberculosis - genetics
Mycobacterium tuberculosis - growth & development
Tuberculosis, Multidrug-Resistant - drug therapy
Tuberculosis, Multidrug-Resistant - microbiology
Tuberculosis, Pulmonary - drug therapy
Tuberculosis, Pulmonary - microbiology
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Summary:We identified a novel 6-benzyl ether benzoxaborole with potent activity against 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 [IC ] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC > 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