TABLE 2.
Effects of CBR-2092 and comparator agents on the in vitro activity of target enzymes from S. aureus
| Test agent | IC50 (μM) forσA RNA polymerase
|
CC50 (μM) for:
|
CC50 ratio for type II DNA topoisomerases
|
|||||
|---|---|---|---|---|---|---|---|---|
| Rifs (RpoBWT)a | Rifr (RpoBH481Y) | DNA topoisomerase IV
|
DNA gyrase
|
GyrAWT/ParCWT | ParCS80F/ParCWT | |||
| ParCWT | ParCS80F | GyrAWT | GyrAS84LParCWT | |||||
| CBR-2092 | 0.034 | >25 | 1.7 | 2.7 | 1.5 | >150 | 0.9 | 1.6 |
| Rifampin | 0.015 | >25 | NRb | NR | NR | NR | NR | NR |
| Ciprofloxacin | NR | NR | 0.4 | 31 | 4.6 | >150 | 11.5 | 77.5 |
| Gatifloxacin | NR | NR | 0.22 | 13 | 0.7 | 18 | 3.2 | 59.1 |
| ABT-719 | NR | NR | 0.06 | 1.1 | 0.09 | 0.9 | 1.5 | 18.3 |
WT, wild type.
NR, not relevant.