The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis.
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We identified a series of novel 7-phenyl benzoxaborole compounds with activity against Mycobacterium tuberculosis. Compounds had a range of activity with inhibitory concentrations (IC90) as low as 5.1 μM and no cytotoxicity against eukaryotic cells (IC50 > 50 μM). Compounds were active against intracellular mycobacteria cultured in THP-1 macrophages. We isolated and characterized resistant mutants with mutations in NADH dehydrogenase (Ndh) or the regulatory protein Mce3R. Mutations suggest that Ndh may be the target of this series.
author list (cited authors)
Korkegian, A., O'Malley, T., Xia, Y. i., Zhou, Y., Carter, D. S., Sunde, B., ... Parish, T
complete list of authors
Korkegian, Aaron||O'Malley, Theresa||Xia, Yi||Zhou, Yasheen||Carter, David S||Sunde, Bjorn||Flint, Lindsay||Thompson, Dean||Ioerger, Thomas R||Sacchettini, Jim||Alley, MRK||Parish, Tanya