Table 4.
Activity of riminophenazine analogs against intracellular M. tuberculosis H37Rv
| Compound | Inhibition (%)a at: |
||
|---|---|---|---|
| 1 μg/ml | 0.5 μg/ml | 0.25 μg/ml | |
| TBI-161 | 99.0 ± 2.1 | 81.8 ± 3.6 | 54.7 ± 1.7 |
| TBI-166 | 93.6 ± 4.6 | 58.1 ± 0.5 | 10.6 ± 1.1 |
| TBI-416 | 100.0 ± 1.6 | 98.0 ± 5.2 | 92.5 ± 3.8 |
| TBI-443 | 99.9 ± 2.4 | 100.1 ± 4.1 | 92.7 ± 0.7 |
| TBI-444 | 99.6 ± 3.1 | 101.4 ± 6.4 | 98.2 ± 0.8 |
| TBI-449 | 99.5 ± 2.4 | 94.7 ± 6.2 | 58.7 ± 2.1 |
| TBI-450 | 99.4 ± 2.4 | 98 ± 5.1 | 72.1 ± 0.8 |
| TBI-678 | 99.9 ± 1.1 | 99.2 ± 4.3 | 68.3 ± 4.7 |
| TBI-688 | 99.7 ± 3.0 | 65.1 ± 2.1 | 61.5 ± 2.7 |
| TBI-1002 | 95.0 ± 5.8 | 96.2 ± 2.1 | 53.4 ± 0.4 |
| TBI-1004 | 97.3 ± 5.2 | 77.2 ± 10.3 | 29.2 ± 3.1 |
| TBI-1010 | 99.7 ± 3.4 | 100.2 ± 0.5 | 96.0 ± 1.2 |
| CFM | 99.5 ± 1.1 | 50.8 ± 5.3 | 7.3 ± 0.3 |
| RIF | 98.2 ± 3.3 | 98.8 ± 3.5 | 93.1 ± 3.9 |
| INH | 94.5 ± 2.7 | 89.5 ± 10.7 | 40.4 ± 1.4 |
a
Variability in background fluorescence accounts for inhibition values of >100%.