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：

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 03期

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.

引用

页码：507 / 514

页数：8

共 11 条

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