The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis.

ABSTRACT: 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.

SUBMITTER: Korkegian A 

PROVIDER: S-EPMC5854369 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature