5-Lipoxygenase inhibitors

Abstract

Ether containing compounds are claimed as inhibitors of 5-lipoxygenase (5-LO), useful in treating allergic and inflammatory diseases. Data are given for 11 compounds in an in vitro assay of inhibition of calcium ionophore-induced LTB₄ biosynthesis in human whole blood. In US5268379 (101] the syntheses of 22 compounds are described as examples, and the structure of an additional 24 compounds are described in a table. Two particularly preferred and specifically claimed compounds are 4-methoxy-4-[3-(1,2-dihydro-1-methyl-2-oxoquinolin-6-yl)methoxy)-trans-prop-1-enyi]tetra hydropyran (1) and 3-(4-methoxytetrahydropyran-4-yl)-N-[(1,2-dihydro-1-methyl-2-oxoquinolin-6-yl)met hyll-trans-propenyl amide (2).