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

Nipul Patel | Zendy; Theresa O’Malley | Zendy; Yong-Kang Zhang | Zendy; Yi Xia | Zendy; Bjorn Sunde | Zendy; Lindsay Flint | Zendy; Aaron Korkegian | Zendy; Thomas R. Ioerger | Zendy; J.C. Sacchettini | Zendy; M.R. Alley | Zendy; Tanya Parish | Zendy

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

Author(s) -

Nipul Patel,

Theresa O’Malley,

Yong-Kang Zhang,

Yi Xia,

Bjorn Sunde,

Lindsay Flint,

Aaron Korkegian,

Thomas R. Ioerger,

J.C. Sacchettini,

M.R. Alley,

Tanya Parish

Publication year - 2017

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.01205-17

Subject(s) - mycobacterium tuberculosis , minimum inhibitory concentration , in vitro , ic50 , ether , microbiology and biotechnology , cytotoxicity , mutant , chemistry , intracellular , bacteria , mycobacterium , pharmacology , tuberculosis , biology , biochemistry , medicine , organic chemistry , gene , genetics , pathology

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 [IC 50 ] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC 50 > 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.

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