The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis | Academic Article individual record
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.

author list (cited authors)
Korkegian, A., O'Malley, T., Xia, Y. i., Zhou, Y., Carter, D. S., Sunde, B., ... Parish, T.
publication date
2018
publisher
Elsevier BV Publisher
published in
TUBERCULOSIS Journal
keywords
  • Bacterial ProteinsBoron CompoundsBridged Bicyclo Compounds, HeterocyclicDose-Response Relationship, DrugDrug Resistance, BacterialHumansMicrobial Sensitivity TestsMutationMycobacterium TuberculosisNadh DehydrogenaseThp-1 Cells