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Target inhibition by tricyclic NBTIs
| Compound | S. aureus DNA gyrase IC50 (nM) a | S. aureus TopoIV IC50 (nM) b |
|---|---|---|
| 1a | 150 | 653 |
| 1b | 229 | 755 |
| 2a c | 1,600 | 1,300 (n = 5) |
| 2b c | 4,200 | 1,400 |
| Gepotidacin (racemic) c | 170 | 2,800 |
| Ciprofloxacin c | 28,000 | 8,600 |
DNA gyrase supercoiling inhibition assay; n = 2.
TopoIV decatenation inhibition assay; n = 2 unless otherwise noted in parentheses.
Values for amine analogs, gepotidacin, and ciprofloxacin were previously reported (21).
