Novel 2-oxoamide inhibitors of human group IVA phospholipase A2

被引：68

作者：

Kokotos, G

Kotsovolou, S

Six, DA

Constantinou-Kokotou, V

Beltzner, CC

Dennis, EA

机构：

[1] Univ Athens, Dept Chem, Organ Chem Lab, Athens 15771, Greece

[2] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

[3] Agr Univ Athens, Chem Labs, Athens, Greece

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 14期

关键词：

D O I：

10.1021/jm025538p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of potent human cytosolic phospholipase A(2) (GIVA PLA(2)) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a long-chain 2-oxoamide containing L-gamma-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA2 activity at 0.009 mole fraction.

引用

收藏

页码：2891 / 2893

页数：3

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