Design, synthesis and cardioprotective effect of a new class of dual-acting agents:: Phenolic tetrahydro-β-carboline RGD peptidomimetic conjugates

被引：35

作者：

Bi, Wei ^{[1
]}

Cai, Jianhui

Liu, Sanguang

Baudy-Floc'h, Michele

Bi, Lanrong

机构：

[1] HeBei Med Univ, Second Hosp, Shijiazhuang 050000, Peoples R China

[2] Michigan Technol Univ, Dept Chem, Houghton, MI 49931 USA

[3] Univ Rennes 1, CNRS, UMR 6226, F-35042 Rennes, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 22期

关键词：

dual-acting agents; phenolic tetrahydro-beta-carboline RGD; peptidomimetics conjugates; free radicals scavenger; antithrombotic agent;

D O I：

10.1016/j.bmc.2007.08.022

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

In this study, a new class of phenolic tetrahydro-beta-carboline RGD peptidomimetic conjugates was designed and synthesized. The radical scavenging activities of these newly synthesized compounds 12a-c were evaluated in PC 12 cell survival assays. The NO scavenging activities of these compounds were confirmed in the acetylcholine-induced vasorelaxation assay. Compounds 12a-c were efficacious in a rat arterial thrombosis model, and were active in ADP- or PAF-induced in vitro platelet aggregation assays, which Suggests these compounds also possess anti-thrombotic activity. The beneficial effects of dual-acting agent 12c were demonstrated on the ischemia-reperfusion induced cardiac infarct size and oxidative change in an in vivo rat model. (C) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：6909 / 6919

页数：11

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