3-(3,5-dimethyl-4-octadecanoylpyrrol-2-yl)propionic acids as inhibitors of 85 kDa cytosolic phospholipase A(2)

被引：10
|
作者：
Lehr, M
机构：
[1] Inst. F. Pharm. Lebensmittelchemie, Ludwig-Maximilians-Universität, D-80333 München
来源：
ARCHIV DER PHARMAZIE | 1996年 / 329卷 / 11期
关键词：
3-(pyrrol-2-yl)propionic acids; 1-acylation of pyrroles; cytosolic phospholipase A(2) inhibitors;
D O I：
10.1002/ardp.19963291103
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
3-(1,4-Diacylpyrrol-2-yl)propionic acids were designed as inhibitors of cytosolic phospholipase A(2). Enzyme inhibition was assayed by evaluation of calcium ionophore A23187-induced arachidonic acid release from bovine platelets. While the synthesized bisacyl compound 3-[3,5-dimethyl-4-octadecanoyl-1-(3-pheylpropionyl)pyrrol-2-yl]propionic acid was inactive at 33 mu M. the related monoacylated 3-(3,5-dimethyl-4-octadecanoylpyrrol-2-yl)-propionic acid and 3-(1,3,5-trimethyl-4-octadecanoylpyrrol-2-yl)-propionic acid proved to be inhibitors of cytosolic phospholipase A(2) (IC50: 24 mu M and 13 mu M, respectively).
引用
收藏
页码：483 / 488
页数：6
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