Table 3. Garenoxacin (36) and two analogs differently substituted at C-6 and C-8. Ciprofloxacin 15 was used as control. Within this panel, 37 is most potent analog against eukaryotic topo II and against human cells.
| Compound | E. coli gyrase IC50 (μg/ml) |
S. aureus topo IV
IC50 (μg/ml) |
topo II DNA relax.
IC50 (μg/ml) |
HEp-2
CC50 (μg/ml) |
HeLa
CC50 (μg/ml) |
|
|---|---|---|---|---|---|---|
|
36 garenoxacin |
0.17 | 2.19 | 509.7 | >166 | >166 | |
| 37 | 0.16 | 4.6 | 128.1 | 41.1 | 203 | |
| 38 | 0.19 | 2.04 | 89.2 | 8.2 | 10.0 | |
|
15 ciprofloxacin |
0.18 | 2.34 | 873 | 115 | 94.2 | |