Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors

Article abstract of DOI:10.1016/S0968-0896(96)00265-9

A series of substituted indolylalkoxyiminoalkylcarboxylates were found to be potent leukotriene biosynthesis inhibitors. The structure-activity relationships were investigated. Representative potent inhibitors identified were the quinolyl 3a (A-86885) and pyridyl 3b (A-86886) congeners with in vitro IC₅₀s of 21 and 9 nM and in vivo leukotriene inhibition in the rat with oral ED₅₀s of 0.9 and 1.7 mg/kg, respectively.