SYNTHESIS AND PLATELET-ACTIVATING-FACTOR (PAF)-ANTAGONISTIC ACTIVITIES OF 1,4-DISUBSTITUTED PIPERAZINE DERIVATIVES

被引：0
|
作者：
FUKUSHI, H
MABUCHI, H
ITOH, K
TERASHITA, Z
NISHIKAWA, K
SUGIHARA, H
机构：
[1] TAKEDA CHEM IND LTD, PHARMACEUT RES LABS 2, YODOGAWA KU, OSAKA 532, JAPAN
[2] TAKEDA CHEM IND LTD, PHARMACEUT RES LABS 3, YODOGAWA KU, OSAKA 532, JAPAN
[3] TAKEDA CHEM IND LTD, DIV PHARMACEUT RES, OSAKA 532, JAPAN
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1994年 / 42卷 / 03期
关键词：
PAF ANTAGONIST; STRUCTURE ACTIVITY RELATIONSHIP; 1,4-DISUBSTITUTED PIPERAZINE; 1-(6-METHOXY-3,4-DIHYDRO-2-NAPHTHOYL)-4-(3,4,5-TRIMETHOXYBENZYL)PIPERAZINE; 1-(2,3-DIMETHOXY-6,7-DIHYDRO-5H-BENZOCYCLOHEPTEN-8-YLCARBONYL)-4-(3,4,5-TRIMETHOXYBENZOYL)PIPERAZINE;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
During the screening of novel platelet-activating factor (PAF) antagonists, we found that 1-(6-methoxy-3,4-dihydro-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine and its 4-(3,4,5-trimethoxybenzoyl)piperazine derivatives (1b, 2b) exerted in vitro and in vivo PAF-antagonistic activities. Modifications of the 1-acyl group, the substituent at the 4-position and the piperazine ring of 1a and 2b were examined and from this series 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8-ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)piperazine (2g) was found to be one of the most potent PAF antagonists.
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页码：541 / 550
页数：10
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