Comparison of the inhibitory activities (IC50, μM) of (R)- and (S)-configuration of selected benzoxaborolesa.
| Cpd ID | Class A KPC-2 | Class C AmpC | Class D OXA-48 | Class B1 NDM-1 | Class B1 IMP-1 | Class B1 VIM-1 | Class B1 VIM-2 |
|---|---|---|---|---|---|---|---|
| (R)-4a | 3.08 | 134.10 | 15.84 | 549.80 | >600 | >600 | 225.40 |
| (S)-4a | 0.48 | 185.7 | 14.06 | >600 | 142.5 | 308.6 | 12.05 |
| (R)-4c | 7.62 | 178.20 | 42.52 | >600 | >600 | >600 | 232.60 |
| (S)-4c | 0.54 | 74.14 | 34.15 | 169.7 | >600 | 466.3 | 22.40 |
| (R)-4f | 3.87 | 140.90 | 10.13 | >600 | 65.65 | 513.8 | 82.80 |
| (S)-4f | 0.34 | 149.8 | 14.68 | 325.3 | 46.5 | >600 | 120.5 |
| (R)-4j | 0.97 | 140.50 | 5.97 | >600 | >600 | >600 | 55.87 |
| (S)-4j | 0.49 | 108.7 | 12.03 | 719.1 | 142.5 | 308.6 | 105.7 |
| (R)-4q | 0.07 | 18.38 | 0.43 | 260.00 | 497.36 | 388.3 | 57.37 |
| (S)-4q | 0.01 | 22.52 | 0.74 | 34.06 | >600 | >600 | 58.49 |
| Avibactam | 0.004 | 0.24 | 0.17 | >600 | 425 | >600 | 19.08 |
a
All tested compounds were recrystallised. IC50 curves are shown in ESI Fig. S1.