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. Author manuscript; available in PMC: 2015 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2014 Jan 3;22(3):1163–1175. doi: 10.1016/j.bmc.2013.12.027

Table 1.

Inhibition of human sEH by substituted oxyoxalamide derivatives

graphic file with name nihms628340u1.jpg
No. R R1 R2 Human sEH IC50 (nM)a
3 graphic file with name nihms628340t1.jpg graphic file with name nihms628340t2.jpg H >10,000
4 graphic file with name nihms628340t3.jpg graphic file with name nihms628340t4.jpg H >10,000
5 graphic file with name nihms628340t5.jpg graphic file with name nihms628340t6.jpg H 838
6 graphic file with name nihms628340t7.jpg graphic file with name nihms628340t8.jpg H 50
7 graphic file with name nihms628340t9.jpg graphic file with name nihms628340t10.jpg H >10,000
8 graphic file with name nihms628340t11.jpg graphic file with name nihms628340t12.jpg H 1500
9 graphic file with name nihms628340t13.jpg graphic file with name nihms628340t14.jpg H >10,000
10 graphic file with name nihms628340t15.jpg graphic file with name nihms628340t16.jpg H 2300
11 graphic file with name nihms628340t17.jpg graphic file with name nihms628340t18.jpg H 4400
12 graphic file with name nihms628340t19.jpg graphic file with name nihms628340t20.jpg H 550
13 graphic file with name nihms628340t21.jpg graphic file with name nihms628340t22.jpg CH3 3200
14 graphic file with name nihms628340t23.jpg CH3 CH3 >10,000
15 graphic file with name nihms628340t24.jpg graphic file with name nihms628340t25.jpg H >10,000
a

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.