Table 2.
Pseudomonas quinolone signaling receptor (PqsR) inverse agonistic activity and pyocyanin inhibitory activity as well as kinetic solubility and metabolic stability of compounds 7–13
| |||||
|---|---|---|---|---|---|
| R | IC50 PqsR [×10−9 m] | IC50 Pyocyanin [×10−6 m] | Solubility [×10−6 m] | MLM t 1/2 [min] a) | |
| 7 |
|
101 ± 37.3 | 0.449± 0.074 | 10 | >40 |
| 8 |
|
210 ± 125 | 3.3 ± 1.3 | 38.9 | 50 |
| 9 |
|
179 ± 103 | 2.9 ± 3.9 | 26.6 | 57 |
| 10 |
|
435 ± 198 | 35.1 ± 27.5 | >200 | 75 |
| 11 |
|
131 ± 9.3 | 7.2 ± 4.6 | 160.7 | >480 |
| 12 |
|
818 ± 436 | >20 | 48.1 | 74 |
| 13 |
|
158 ± 36.1 | 3.1 ± 0.9 | 42.3 | 6 |
Bi‐aryl core optimization.
a)
Half‐life against mouse liver microsomes (MLM).