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In vitro inhibition (apparent IC50) of bacterial DHFR by select DADHTs.
| Compound |
EcDHFR IC50 (μM ± SD) |
SaDHFR IC50 (μM ± SD) |
|---|---|---|
| CYC | 23 ± 16 | nfa |
| 1d | 3 ± 1 | ntb |
| 1e | 1.0 ± 0.3 | 2.5 ± 0.5 |
| 1f | 5 ± 2 | nt |
| 2f | 26 ± 9 | 14 ± 5 |
| 3c | 3 ± 1 | nt |
| 3d | 5 ± 3 | 1.7 ± 0.3 |
| 3e | 2.1 ± 0.2 | 0.9 ± 0.3 |
| 5 | 7 ± 5 | 23 ± 14 |
| TMP | 9.9 × 10−3 ± 7 × 10−3 | 3.3 × 10−3 ± 7 × 10−4 |
nf = no fit to the data due to partial inhibition, see Figure S17 and S18.
nt = not tested.
