TABLE 2.
In vitro activity of selected sPBTZ derivatives against M. tuberculosis H37Rv and its BTZ-resistant mutant (NTB1), and cytotoxicity for HepG2 cells
| Compound | MIC99 (μg/ml) |
TD50 (μg/ml) | Selective index | |
|---|---|---|---|---|
| H37Rv | NTB1 | |||
| 11326059 | 0.004 | >100 | 100 | 25,000 |
| 11326127 | 0.006 | >100 | >100 | >16,666 |
| 11626091 | 0.003 | 14.7 | 8.10 | 2,700 |
| 11626092 | 0.003 | 25.1 | 8.90 | 2,967 |
| 11626093 | 0.001 | >100 | >100 | >100,000 |
| 11626094 | 0.01 | >100 | 100.00 | 10,000 |
| 11626095 | 0.02 | 75 | 7.80 | 390 |
| PBTZ169 | 0.0002 | >100 | 44.00 | 220,000 |
| Rifampin | 0.0008 | 0.0008 | 100.00 | 125,000 |