DESIGN OF PYRROLO-1,4-BENZOXAZINE DERIVATIVES AS INHIBITORS OF 5-LIPOXYGENASE AND PAF ANTAGONISTS WITH ANTIHISTAMINIC PROPERTIES

被引:6
作者
DEMONCHAUX, P
LENOIR, P
AUGERT, G
DUPASSIEUX, P
机构
[1] Solvay Pharma, Laboratoires de Thérapeutique Moderne
关键词
D O I
10.1016/S0960-894X(01)80395-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 5-hydroxyphenylpyrrolo-1,4-benzoxazine derivatives substituted by a pyridinylpiperazinyl alkyl chain were designed as multimediator compounds with potential antiasthmatic properties. These compounds were prepared and evaluated both in vitro against leukotriene synthesis and PAF activity and in vivo against histamine. Structure-activity relationships led to compound 11 which displayed the most potent activities in this series.
引用
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页码:2383 / 2388
页数:6
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