Table 1. Inhibitory Activity (IC50, μM) of Rhodanines against Four MβLs in 50 mM Tris-HCl, pH 7.0a.
B1 |
B2 | B3 | B1 |
B2 | B3 | ||||
---|---|---|---|---|---|---|---|---|---|
compd | NDM-1b | VIM-2b | ImiSc | L1b | compd | NDM-1b | VIM-2b | ImiSc | L1b |
1a | 0.32 ± 0.02 | 2b | 0.69 ± 0.02 | 0.18 ± 0.02 | |||||
1b | 47 ± 1 | 1.7 ± 0.1 | 2c | 14.3 ± 0.4 | 0.59 ± 0.02 | ||||
1c | 0.77 ± 0.09 | 2d | 1.13 ± 0.06 | 0.92 ± 0.02 | 0.21 ± 0.02 | ||||
1d | 19.1 ± 0.6 | 0.16 ± 0.03 | 2e | 1.9 ± 0.3 | 16.5 ± 0.3 | 0.12 ± 0.01 | |||
1e | 0.37 ± 0.01 | 2f | 6.9 ± 0.2 | 0.10 ± 0.01 | |||||
1f | 27.9 ± 0.3 | 0.28 ± 0.01 | 2g | 12 ± 1 | 15.0 ± 0.3 | 0.31 ± 0.02 | |||
1g | 25.1 ± 0.8 | 0.6 ± 0.1 | 2h | 12.2 ± 0.9 | 3.6 ± 0.1 | 7.7 ± 0.9 | 0.070 ± 0.002 | ||
1h | 15.3 ± 0.8 | 0.22 ± 0.06 | 2i | 10.6 ± 0.8 | 3.5 ± 0.2 | 7.6 ± 0.2 | 0.030 ± 0.008 | ||
1i | 21.5 ± 0.8 | 25.1 ± 0.4 | 0.080 ± 0.002 | 2j | 8.4 ± 0.4 | 6.9 ± 0.2 | 3.6 ± 0.1 | 0.080 ± 0.003 | |
1j | 15.4 ± 0.9 | 14.4 ± 0.6 | 0.20 ± 0.02 | 2k | 10.6 ± 0.5 | 2.36 ± 0.09 | 7.8 ± 0.5 | 0.070 ± 0.008 | |
1k | 14.3 ± 0.9 | 12.7 ± 0.9 | 0.11 ± 0.02 | 2l | 1.31 ± 0.05 | 0.19 ± 0.03 | 3.0 ± 0.2 | 0.050 ± 0.003 | |
1l | 27.4 ± 0.4 | 16.8 ± 0.4 | 0.22 ± 0.01 | 2m | 6.7 ± 0.2 | 3.9 ± 0.3 | 15.9 ± 0.8 | 0.020 ± 0.004 | |
1m | 0.10 ± 0.01 | 3a | 4.7 ± 0.4 | 0.32 ± 0.01 | |||||
2a | 8.7 ± 0.9 | 18.3 ± 0.2 | 0.21 ± 0.01 |
Blank spaces represent percent inhibition under 50% at a concentration of 50 μM.
The antibiotic used was cefazolin.
The antibiotics used was imipenem.