Table 2. Biological Activity of Chloroacetamide and Maleimide Analogues.
| compd | IC50 (μM)a | % inhibition at 100 μMb |
|---|---|---|
| 17 | 73.8 ± 19.4 | 91 |
| 18 | 99.5 ± 21.0 | 79 |
| 24 | 86.8 ± 57.4 | 56 |
| 25 | 3.6 ± 1.9 | 98 |
| 26 | 78.1 ± 69.3 | 30 |
| 27 | 51.9 ± 35.1 | 32 |
| 28 | 1.5 ± 0.5 | 101 |
a
Values determined employing the GFP-based LasR antagonist bioassay (see Supporting Information). All IC50 values are reported as the mean of triplicate analysis with the range defining the 95% confidence interval. Br-HSL (4) was used as a control for antagonism with an IC50 = 16.4 ± 7.4 μM.
b
Percent inhibition of GFP at 100 μM with respect to Br-HSL (4) as a positive control for LasR antagonism, set at 100% inhibition.