Table 1.
IC50 values for LasR inhibition by selected compounds in P. aeruginosa PAO-JP2 and PAO-JG21.a
| PAO-JP2 | PAO-JG21 | ||||
|---|---|---|---|---|---|
| Compound | IC50 (µM) | 95% CI (µM) | IC50 (µM) | 95% CI (µM) | Fold change of IC50 |
| A4 | 1.0b | 0.21–4.9 | 0.12b | 0.021–0.70 | 8.3 |
| B14 | 15b | 2.9–34 | 0.95b | 0.43–2.1 | 15 |
| E5 | 12 | 6.5–21 | 3.1 | 2.6–3.8 | 3.9 |
| E6 | ≥ 480 | - | 19 | 12–33 | ≥ 25 |
| E32 | 6.0 | 3.2–11 | 0.26b | 0.043–1.5 | 23 |
| E33 | 15b | 9.1–24 | 0.20b | 0.062–0.65 | 75 |
| E35 | 5.7b | 1.7–19 | 0.16b | 0.061–0.40 | 35 |
| E36 | 14b | 2.5–81 | 0.34b | 0.11–1.1 | 41 |
| R4 | ≥ 570 | - | 41 | 30–57 | ≥ 13 |
| R5 | ≥ 230 | - | 55 | 38–78 | ≥ 4.2 |
| S1 | ≥ 710 | - | 24 | 16–34 | ≥ 29 |
| 3-oxo-C12-aniline | 11 | 4.2–23 | 1.7 | 1.3–4.2 | 6.5 |
| DMABI | 2.3 | 1.3–4.1 | 1.4 | 0.81–2.5 | 1.6 |
[a]
Antagonism assays were performed in the presence of 100 nM OdDHL in PAO-JP2 and 10 nM OdDHL in PAO-JG21.
[b]
Antagonism dose response exhibited non-monotonic behavior, showing an increase in activity at high concentrations. We have previously identified this phenomenon,[11d] and studies are currently underway to identify the mechanistic basis for the trend.