Novel 3,5-diaryl pyrazolines and pyrazole as low-density lipoprotein (LDL) oxidation inhibitor

被引：96

作者：

Jeong, TS ^{[1
]}

Kim, KS ^{[1
]}

Kim, JR ^{[1
]}

Cho, KH ^{[1
]}

Lee, S ^{[1
]}

Lee, WS ^{[1
]}

机构：

[1] Korea Res Inst Biosci & Biotechnol, Natl Res Lab Lipid Metab & Atherosclerosis, Taejon 305333, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

关键词：

LDL-antioxidant;

D O I：

10.1016/j.bmcl.2004.03.072

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Compounds 4a-j and 5 were synthesized by cyclocondensation of 3a-j and hydrazine and showed significant LDL-antioxidant activities in the TBARS assay, the lag time of conjugated diene production, the relative electrophoretic mobility (REM) of ox-LDL, the apoB-100 fragmentation, and the macrophage-mediated LDL oxidation. Among compounds 4a-j and 5, 4a was found to be the most active compound as an inhibitor of LDL oxidation and 4a (IC50 = 0.1 muM) was 6-fold more potent than probucol (IC50 = 0.6 muM) in the TBARS assay. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：2719 / 2723

页数：5

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