Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors

被引:8
作者
Kolasa, T
Bhatia, P
Brooks, CDW
Hulkower, KI
Bouska, JB
Harris, RR
Bell, RL
机构
关键词
D O I
10.1016/S0968-0896(96)00265-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of substituted indolylalkoxyiminoalkylcarboxylates were found to be potent leuko triene 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 IC(50)s of 21 and 9 nM and in vivo leukotriene inhibition in the rat with oral ED(50)s of 0.9 and 1.7 mg/kg, respectively. (C) 1997 Elsevier Science Ltd.
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页码:507 / 514
页数:8
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