TABLE 2.
Poisoning of E. coli gyrase and Topo IV
| Compound | Median CC3 (μM) ± AD |
||||
|---|---|---|---|---|---|
| Wild-type gyrase | GyrA S83W gyrase | GyrA G81C gyrase | GyrA A67S gyrase | Topo IV | |
| Ciprofloxacin | 0.097 ± 0.003 | 39 ± 5.0 (402)a | 3.2 ± 0.7 (33) | 0.28 ± 0.05 (2.9) | 14.2 ± 3.3 |
| 8-Methoxy fluoroquinolone | 0.023 ± 0.001 | 0.15 ± 0.01 (6.5) | 0.30 ± 0.02 (13) | 0.035 ± 0.004 (1.5) | 1.4 ± 0.2 |
| 8-Methoxy 2,4-dione | 0.52 ± 0.04 | 1.1 ± 0.22 (2.1) | 1.2 ± 0.04 (2.3) | 0.88 ± 0.1 (1.7) | 11.1 ± 1.9 |
| 8-Methyl 2,4-dione | 0.13 ± 0.02 | 0.73 ± 0.02 (5.6) | 0.41 ± 0.02 (3.1) | 0.33 ± 0.05 (2.5) | 3.0 ± 0.2 |
| 5-Methoxy 1,3-dione | 3.8 ± 0.2 | 13 ± 2.2 (3.4) | 8.9 ± 1.6 (2.3) | 5.8 ± 1.0 (1.5) | 108 ± 8.0 |
a
The ratio of the CC3 value for a mutant gyrase to that for the wild-type gyrase is shown in parentheses.