Table 2. Inhibition of 5-LOX Product Formation in Activated PMNL of Human Isolated 5-LOX and Human Isolated sEH^a,b.

compound	R1	X	IC50 in PMNL (μM)	IC50 for isolated 5-LOX (μM)	IC50 for isolated sEH (μM)
43	4-F-PhCH2-		1.38 ± 0.23	0.45 ± 0.11	1.39 ± 0.45
21	4-F-PhCH2-		>10	>10	>10
44	4-F-PhCH2CH2-		4.87 ± 0.41	0.38 ± 0.05	1.14 ± 0.29
45	4-Ph-PhCH2-		>10	1.48 ± 0.48	>10
46	β-NaphthylCH2-		>10	1.02 ± 0.44	0.91 ± 0.24
48	HO(CH2)3CH2-		nd	9.02 ± 4.20	13.86 ± 1.60
49	4-CH3OCH2O-PhCH2-		2.93 ± 0.70	>10	2.40 ± 0.80
50	(CH3)3CCH2-	NH	>10	1.42 ± 0.23	>10
51	H2N(CH2)3CH2-		>10	>10	>10
52	4-HO-PhCH2-		2.90 ± 0.75	5.10 ± 2.92	0.79 ± 0.52
53	Cyclohexyl-	O	>10	0.28 ± 0.02	0.061 ± 0.003
54	(CH3)3CCH2-	O	nd	0.18 ± 0.05	0.10 ± 0.01
56	PhCH2-	S	0.95 ± 0.15	0.57 ± 0.12	3.86 ± 0.79
57	Ph-	S	1.98 ± 0.32	0.16 ± 0.05	10.39 ± 0.37
58	4-COOH-Ph-	S	>10	2.29 ± 0.46	>10
68	4-F-PhCO-		>10	>10	>10
69	4-F-PhCH2CO-		>10	>10	>10
73	4-ONPhCH2-		0.59 ± 0.09	0.41 ± 0.01	0.43 ± 0.10
77	(CH3)3CCH2-		>10	>10	2.12 ± 1.06
82	(CH3)3CCH2-		>10	>10	>10

^aAll values are given as the mean ± SEM of single determinations obtained in 3–4 independent experiments.

^bZileuton used as a positive control at 3 μM gives residual activities of 3.90 ± 4.14 and 14.24 ± 5.88% over PMNL and isolated 5-LOX, respectively. AUDA used as a positive control at 1 μM gives a residual activity of 3.90 ± 4.14% over isolated sEH.

^cnd, not determined.