Design, synthesis, and biological activities of novel Ligustrazine derivatives

被引：42

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

页码：3315 / 3320

页数：6

共 12 条

[1] Experimental study on anticoagulant and antiplatelet aggregation activity of a chemically sulfated marine polysaccharide YCP [J].