Table 1. New inhibitors of PBPs from resistant bacteria.a .
Compound | PBP2a RA [%] (IC50) | PBP2x5204 RA [%] (IC50) | PBP5fm RA [%] (IC50) |
1 | 0 (97 µM) | 38b (391 µM) | 100 |
2 | 58 | 123 | 39 (930 µM) |
3 | 67 | 80 | 65 |
4 | 83 | 101 | 100 |
5 | 86 | 81 | 73 |
6 | 0 (210 µM) | 41 | 68 |
7 | 74 | 65 | 72 |
8 | 60 | 103 | 74 |
9 | 0 (230 µM) | 8b (155 µM) | 72 |
10 | 17 (680 µM) | 121 | 69 |
11 | 70 | 118 | 61 |
12 | 47 (910 µM) | 97 | 34 (>1 mM) |
The data represent mean values of three independent experiments. Standard deviations were within ±10% of these mean values. RA = residual activity of the enzyme at 1 mM inhibitor, unless stated otherwise. IC50-values were determined in the presence of 0.01% Triton X-100. bResidual activity of the enzyme at 500 µM inhibitor.