STUDIES ON CEREBRAL PROTECTIVE AGENTS .2. NOVEL 4-ARYLPYRIMIDINE DERIVATIVES WITH ANTI-ANOXIC AND ANTILIPID PEROXIDATION ACTIVITIES .2.

被引:0
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作者
KUNO, A
SUGIYAMA, Y
KATSUTA, K
SAKAI, H
TAKASUGI, H
机构
关键词
CEREBRAL PROTECTIVE AGENT; 4-ARYLPYRIMIDINE; 4-ARYL-1,4-DIHYDROPYRIMIDINE; ANTIANOXIA; ANTILIPID PEROXIDATION; CEREBRAL EDEMA; STRUCTURE-ACTIVITY RELATIONSHIP; FK360;
D O I
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl)-2-phenylpyrimidine (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. Structure-activity relationships in regard to AA activity of this series of compounds are also discussed.
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页码:2423 / 2431
页数:9
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