Table 3.

Pseudomonas quinolone signaling receptor (PqsR) inverse agonistic activity and pyocyanin inhibitory activity as well as kinetic solubility and metabolic stability of compounds 14–25

	R	IC50 PqsR [×10−9 m]	IC50 Pyocyanin [×10−6 m]	Solubility [×10−6 m]	MLM t 1/2 [min] a)
14		235 ± 13	2.9 ± 0.8	>200	77
15		154 ± 79.8	1.9 ± 0.3	112.5	<5
16		176 ± 9.8	2.1 ± 0.4	100.9	384
17		53.9 ± 11.8	0.802 ± 0.2	76.2	45
18		96.8 ± 12.4	1.5 ± 0.2	42.4	2
19		159 ± 13.6	4.2 ± 1.1	25.6	35
20		39.4 ± 2.6	0.234 ± 0.057	16.6	61
21		60.5 ± 11.4	0.32 ± 0.11	10.9	32
22		14.2 ± 4.0	0.521 ± 0.3	41.7	>85
23		61.4 ± 34.9	0.591 ± 0.07	16.5	3
24		27.5 ± 4.7	0.245 ± 0.04	47.2	19
25		43.7 ± 12.7	0.523 ± 0.05	37.9	>480

Identification of the pyrimidine core.

^a) Half‐life against mouse liver microsomes (MLM).