Table 3.
Inhibitory activity of selected compounds against DNA gyrase from S. aureus and topoisomerase IV from E. coli and S. aureus.
| Compd. | IC50 (μM)a or RA (%)b |
||
|---|---|---|---|
| S. aureus gyrase | E. coli topo IV | S. aureus topo IV | |
| 8c | 5.9 ± 0.7 μM | 78% | 98% |
| 8e | 0.093 ± 0.065 μM | 0.45 ± 0.12 μM | 0.28 ± 0.20 μM |
| 8f | 1.6 ± 0.6 μM | 7.4 ± 1.5 μM | 1.3 ± 0.1 μM |
| 8i | 1.3 ± 0.0 μM | 100% | 99% |
| 9b | 0.39 ± 0.09 μM | 89% | 3.7 ± 0.3 μM |
| 9d | 89% | 96% | 98% |
| 9e | 0.11 ± 0.04 μM | 0.53 ± 0.06 μM | 3.2 ± 0.4 μM |
| 10a | 22 ± 10 μM | 100% | 92% |
| 11a | 0.75 ± 0.15 μM | 11 ± 0 μM | 12 ± 0 μM |
| 12 | 1.0 ± 0.3 μM | 0.57 ± 0.16 μM | 0.96 ± 0.09 μM |
| 23a | 79% | 42 ± 11 μM | 39 ± 0 μM |
| 23c | 85% | 100% | 96% |
| 23d | 0.14 ± 0.02 μM | 100% | 12 ± 0 μM |
| novobiocin | 0.041 ± 0.07 μM | 11 ± 2 μM | 27 ± 7 μM |
a
Concentration of compound that inhibits the enzyme activity by 50%.
b
Residual activity of the enzyme at 1 μM of the compound.