Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

被引：13
|
作者：
Jang, Soyong
Jung, Jae-Chul
Oh, Seikwan [1 ]
机构：
[1] Ewha Womans Univ, Sch Med, Dept Neurosci, Seoul 158710, South Korea
[2] Ewha Womans Univ, Sch Med, Med Res Inst, Seoul 158710, South Korea
[3] Univ Mississippi, Sch Pharm, Dept Med Chem, University, MS 38677 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 12期
关键词：
1,3-diphenyl-2-propen-1-ones; Grignard reaction; NO-generation; anti-excitotoxicity;
D O I：
10.1016/j.bmc.2007.03.077
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：
A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 VM in vitro. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4098 / 4105
页数：8
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