Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase

Abstract

Structure and activity relationships of (methoxyalkyl)thiazole and 4-methoxytetrahydropyran series of 5-lipoxygenase inhibitors are reviewed. One member of the 4-methoxytetrahydropyran series, 6-{[fluoro-5-(4-methoxy-3,4,5,6-tetrahydro-2 H-pyran-4-yl)phenoxy]methyl}-1-methylquinol-2-one (ICI D2138), is undergoing clinical evaluation.