Journal
TUBERCULOSIS
Volume 108, Issue -, Pages 96-98Publisher
CHURCHILL LIVINGSTONE
DOI: 10.1016/j.tube.2017.11.003
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Funding
- Bill and Melinda Gates Foundation [OPP1024038]
- NIAID of the National Institutes of Health [R01AI099188]
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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 mu M and no cytotoxicity against eukaryotic cells (IC50 > 50 mu M). 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.
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