1-(5-carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α:: Bioisosteric replacement of the carboxylic acid and carboxamide moiety

被引：24

作者：

Hess, Mark ^{[1
]}

Elfringhoff, Alwine Schulze ^{[1
]}

Lehr, Matthias ^{[1
]}

机构：

[1] Univ Munster, Inst Pharmaceut & Med Chem, D-48149 Munster, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 08期

关键词：

cytosolic phospholipase A(2)alpha inhibitors; indol-1-ylpropan-2-ones; bioisosteric replacement;

D O I：

10.1016/j.bmc.2007.02.016

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Indole-5-carboxylic acids and -carboxamides with 3-aryloxy-2-oxopropyl residues in position I were previously reported to be potent inhibitors of cytosolic phospholipase A(2)alpha (cPLA(2)alpha) isolated from human platelets. In continuation of our attempts to develop novel cPLA(2)alpha inhibitors, a number of derivatives of these substances characterized by bioisosteric replacement of the carboxylic acid and carboxamide functionality, respectively, were prepared. The results of the biological evaluation of the obtained compounds enabled us to gain further insight into structural features critical for cPLA(2)alpha inhibition. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2883 / 2891

页数：9

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