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| IC50 (μM) or RA (%)a |
||||||
|---|---|---|---|---|---|---|
| Cmpd | n | R | E. coli gyrase | E. coli topo IV | S. aureus gyrase | S. aureus topo IV |
| 4a | 0 | Et | 4.0 ± 1.6 μM | 100% | 100% | 100% |
| 4b | 1 | Me | 7.0 ± 3.4 μM | 100% | 100% | 100% |
| 5a | 0 | H | 0.60 ± 0.32 μM | 12 ± 2 μM | 80 ± 23 μM | 31 ± 1 μM |
| 5b | 1 | H | 1.5 ± 0.2 μM | 100% | 100% | 100% |
| 1 | 0.058 μM | 13 μM | >100 μM | 10 μM | ||
| novobiocin | 0.17 μM | 11 μM | 0.041 μM | 27 μM | ||
Residual activity of the enzyme at 10 μM concentration of the compound.
