Fig. 2. B2 and H3 are potent DprE1 inhibitors.
a The antibacterial activity of compound B2 and H3 against M. smegmatis. The TBA-7371 and rifampin were used as positive controls. b Overexpression of Mt-DprE1 in M. smegmatis confers 4-fold, 16-fold, 8-fold and 8-fold increase in resistance to PBTZ169, TBA-7371, H3 and B2, but no resistance to rifampin. The compound concentrations expressed as fold-× of the MIC of each compound. Pink indicates viable cells, and blue indicates nonviable cells. WT strain refers to wild-type M. smegmatis that did not overexpress Mt-DprE1. c The thermal shift melt curves for DprE1 with rifampi. d The thermal shift melt curves for DprE1 with compound B2. e The thermal shift melt curves for DprE1 with PBTZ169. f The thermal shift melt curves for DprE1 with compound H3.
