A-81834

Reference FLAP (five lipoxygenase activating protein) inhibitors MK-886 and MK-0591 were converted into the corresponding O-acetic acid oxime congeners I (R = Me₂CH) and I (R = 2-quinolylmethoxy), resp., resulting in potent, orally active, leukotriene biosynthesis inhibitors.An attempt to create a dual FLAP and direct 5-LO (5-lipoxygenase) inhibitor by replacing the carboxylate group in MK-886 with the N-hydroxyurea pharmacophore did not provide superior inhibitors.