Table 1.
| ||||
---|---|---|---|---|
No. | R | R1 | R2 | Human sEH IC50 (nM)a |
3 | H | >10,000 | ||
4 | H | >10,000 | ||
5 | H | 838 | ||
6 | H | 50 | ||
7 | H | >10,000 | ||
8 | H | 1500 | ||
9 | H | >10,000 | ||
10 | H | 2300 | ||
11 | H | 4400 | ||
12 | H | 550 | ||
13 | CH3 | 3200 | ||
14 | CH3 | CH3 | >10,000 | |
15 | H | >10,000 |
Test compounds prepared in DMSO were reacted with human sEH (1 nM) for 10 min in 25 mM Bis–Tris/HCl buffer (202 μL; pH 7.0) at 30 °C. The fuorescent substrate (CMNPC; [S] = 5 μM) was then introduced to the incubation mixture. Inhibition potency against the human sEH was determined by measuring the appearance of the 6-methoxy-2-naphthaldehyde with an excitation wavelength of 330 nm and an emission wavelength of 465 nm for 10 min on a fluorometer. Results are averages of three separate measurements. See the Supplementary data for the detailed procedures.