Dual-acting agents that possess free radical scavenging and antithrombotic activities:: Design, synthesis, and evaluation of phenolic tetrahydro-β-carboline RGD peptide conjugates

被引：21

作者：

Bi, Wei

Bi, Lanrong

Cai, Jianhui

Liu, Sanguang

Peng, Shiqi

Fischer, Nicholas O.

Tok, Jeffrey B. -H. ^{[1
]}

Wang, Guohua

机构：

[1] Hebei Med Univ, Affiliated Hosp 2, Shijiazhuang 050000, Peoples R China

[2] Capital Univ Med Sci, Coll Pharmaceut Sci, Beijing 100054, Peoples R China

[3] Lawrence Livermore Natl Lab, Chem & Mat Sci Directorate, Livermore, CA 94550 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 17期

关键词：

anti-thrombotic; free radical; dual-action;

D O I：

10.1016/j.bmcl.2006.06.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new approach to construct a single dual-acting agent is described. Compounds 6a-c are potent free radical scavengers as demonstrated by the EC50 values in PC12 cell survival assay in term of NO, H2O2, and (OH)-O-. scavenging activity. The Ach-induced vaso-relaxation assay further confirms the potent NO scavenging activity of compounds 6a-c. In addition, 6a-c are efficacious in a rat arterial thrombosis, and are active in ADP- or PAF-induced in vitro platelet aggregation assay, suggesting that compounds 6a-c also possess anti-thrombotic activities. Since both free radical and thrombogenesis are important risk factors in myocardial ischemic/reperfusion injuries, these dual-acting agents having both free radical scavenging and antithrombolic activities may potentially be beneficial toward their treatment. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4523 / 4527

页数：5

共 38 条

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