Table 1. The inhibitory activities (IC50, μM) of benzenesulfonamide derivatives against MβL ImiS a .
P-Substituted compd. | IC50 | M-Substituted compd. | IC50 | O-Substituted compd. | IC50 |
1a | 7.5 ± 0.3 | 2a | 0.15 ± 0.04 | 3e | 5.4 ± 0.2 |
1b | 2.7 ± 0.4 | 2b | 0.14 ± 0.07 | 3f | 4.6 ± 0.2 |
1c | 4.8 ± 0.1 | 2c | 0.86 ± 0.04 | RS | 6.8 ± 0.5 |
1d | 9.3 ± 0.3 | 2d | 0.31 ± 0.05 | ||
1e | 5.1 ± 0.5 | 2e | 0.44 ± 0.01 | ||
1f | 3.3 ± 0.1 | 2f | 0.23 ± 0.08 | ||
1g | 7.3 ± 0.2 | 2g | 0.11 ± 0.02 | ||
1h | 3.5 ± 0.2 | 2h | 0.16 ± 0.08 | ||
1i | 5.6 ± 0.7 | ||||
1j | 4.1 ± 0.6 |
aThe substrate used was imipenem and inhibitor concentrations were varied between 0.01 and 20 μM. Enzyme and inhibitors were preincubated for 3 h before testing.