TABLE 2

In vitro activity of selected sPBTZ derivatives against M. tuberculosis H37Rv and its BTZ-resistant mutant (NTB1), and cytotoxicity for HepG2 cells

CompoundMIC99 (μg/ml)TD50 (μg/ml)Selective index
H37RvNTB1
113260590.004>10010025,000
113261270.006>100>100>16,666
116260910.00314.78.102,700
116260920.00325.18.902,967
116260930.001>100>100>100,000
116260940.01>100100.0010,000
116260950.02757.80390
PBTZ1690.0002>10044.00220,000
Rifampin0.00080.0008100.00125,000