Table 1.
Pseudomonas quinolone signaling receptor (PqsR) inverse agonistic activity and pyocyanin inhibitory activity as well as kinetic solubility and metabolic stability of compounds 1–6
| |||||
|---|---|---|---|---|---|
| R | IC50 PqsR [×10−9 m] | IC50 Pyocyanin [×10−6 m] | Solubility [×10−6 m] | MLM t 1/2 [min] a) | |
| 1 | – | 2309 | 107 | ||
| 2 |
|
2207 ± 4038 | 176 ± 47.4 | >200 | 54 |
| 3 |
|
1376 ± 735 | 19.0 ± 1.2 | >200 | 44 |
| 4 |
|
861 ± 162 | 14.4 ± 1.6 | >200 | 61 |
| 5 |
|
4955 ± 4850 | 71.4 ± 27.2 | >200 | 20 |
| 6 |
|
>10000 | 126 ± 10.6 | >200 | 4 |
Importance of the NH2 group and identification of growth vector.
a)
Half‐life against mouse liver microsomes (MLM).