TABLE 6.
Inhibition of E. coli DNA gyrase supercoiling by 5,6-bridged dioxinoquinolones and comparator quinolones
| Quinolone | IC50 (μg/ml)a
|
QR/WT ratiob | |
|---|---|---|---|
| WT gyrase | QR gyrase | ||
| PGE-8367769 | 7.5 | 81.3 | 10.8 |
| PGE-6596491 | 62.3 | >500 | — |
| PGE-7872411 | 6.5 | 102.1 | 15.7 |
| PGE-878935 | 6.6 | 77.1 | 11.6 |
| PGE-6116542 | >500 | >500 | — |
| PGE-5215205 | 219.7 | >500 | — |
| PGE-9604297 | 179.5 | >500 | — |
| Nalidixic Acid | 15.9 | >500 | — |
| Ciprofloxacin | 0.12 | 16.1 | 134.3 |
| Clinafloxacin | 0.032 | 0.45 | 13.8 |
a
WT, wild type; QR, quinolone resistant (GyrA S83L).
b
The QR/WT ratio were calculated by dividing the IC50 for the wild-type gyrase by the IC50 for the quinolone-resistant gyrase. —, could not be calculated.