Table 1. Inhibition of 5-LOX Product Formation in Activated PMNL of Human Isolated 5-LOXa,b.
| compound | R | IC50 (μM) in PMNL | IC50 for isolated 5-LOX |
|---|---|---|---|
| 4 | -CH2-4-COOH–Ph- | >10 | >10 |
| 5 | -(CH2)3COOH | >10 | |
| 8 | -(CH2)3NHCOC6F5 | >10 | |
| 10 | -(CH2)3guanidine | >10 | |
| 13 | |||
| 17 | -(CH2)3NH2 | >10 | |
| 18 | -(C-H2)3guanidine | >10 | |
| 43 | -CSNHCH2C(CH3)3 | 1.38 ± 0.45 | 0.45 ± 0.11 |
| 55 | -SO2-cyclohexyl | >10 |
a
The values are given as the mean ± standard error of the mean (SEM) of single determinations obtained in 3–4 independent experiments.
b
Zileuton 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.