Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors.
作者信息
Kolasa T, Bhatia P, Brooks C D, Hulkower K I, Bouska J B, Harris R R, Bell R L
机构信息
Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
出版信息
Bioorg Med Chem. 1997 Mar;5(3):507-14. doi: 10.1016/s0968-0896(96)00265-9.
PMID:9113329
Abstract
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.
摘要
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