Design, synthesis, and biological activities of novel Ligustrazine derivatives

被引：39
|
作者：
Cheng, Xian-Chao
Liu, Xin-Yong
Xu, Wen-Fang
Guo, Xiu-Li
Ou, Yang
机构：
[1] Shandong Univ, Sch Pharmaceut Sci, Inst Mat Chem, Jinan 250012, Peoples R China
[2] Shandong Univ, Sch Pharmaceut Sci, Inst Pharmacol, Jinan 250012, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 10期
关键词：
Ligustrazine; Ligustrazine derivatives; synthesis; cerebrocardiac vascular activity;
D O I：
10.1016/j.bmc.2007.03.033
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 series of novel Ligustrazine derivatives was designed, synthesized, and assayed for their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities. The results showed that most Ligustrazine derivatives exhibited lower EC50 values for protective effects on the ECV-304 cells damaged by hydrogen peroxide in comparison with Ligustrazine. And some Ligustrazine derivatives presented better antiplatelet aggregation activities than Ligustrazine. The derivatives containing the bisphenylmethyl pharmacophore (7a-c) exhibited highest potency. Compound 7a displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound 7c was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3315 / 3320
页数：6
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