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
收藏
页码：3679 / 3681
页数：3
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