The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis

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.

Source: Tuberculosis - November 6, 2017 Category: Respiratory Medicine Authors: Aaron Korkegian, Theresa O'Malley, Yi Xia, Yasheen Zhou, David S. Carter, Bjorn Sunde, Lindsay Flint, Dean Thompson, Thomas R. Ioerger, Jim Sacchettini, M.R.K. Alley, Tanya Parish Source Type: research