Novel δ2-isoxazolines as group II phospholipase A2 inhibitors

被引：40

作者：

Basappa

Kumar, MS

Swamy, SN

Mahendra, M

Prasad, JS

Viswanath, BS

Rangappa, KS ^{[1
]}

机构：

[1] Univ Mysore, Dept Studies Chem, Mysore 570006, Karnataka, India

[2] Univ Mysore, Dept Studies Biochem, Mysore 570006, Karnataka, India

[3] Univ Mysore, Dept Studies Phys, Mysore 570006, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 14期

关键词：

delta(2-)isoxazoline; aldoxime; phospholipase A(2); anti-inflammatory; ursolic acid;

D O I：

10.1016/j.bmcl.2004.05.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesized imidazolyl substituted delta(2)-isoxazolines were subjected to Phospholipase A(2) (PLA(2)) enzyme inhibitory activity against snake venom source and their structure-activity relationship with respect to different groups attached to this moiety is reported for the first time. The crystal structure of the compound 2-butyl-5-chloro-3H-imidazolyl-4-carbaldehyde oxime 2, an intermediate for the construction of isoxazolines is reported. These compounds exerted a significant PLA2 enzyme inhibitory activity against group II PLA2. The in vivo activity on mice of selected compounds 3bI and 3bIV shows the comparable anti-inflammatory activity with the known standard ursolic acid. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3679 / 3681

页数：3

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