Selective peroxisome proliferator-activated receptor δ isosteric selenium agonists as potent anti-atherogenic agents in vivo

被引：9

作者：

Chin, Jungwook ^{[1
]}

Hong, Jun Young ^{[1
]}

Lee, Jaehwan ^{[1
]}

Hwang, Hoosang ^{[1
]}

Ko, Hyunsil ^{[1
]}

Choi, Hyukjae ^{[1
]}

Hahn, Dongyup ^{[1
]}

Ko, Jaeyoung ^{[1
]}

Nam, Sang-Jip ^{[1
]}

Tak, Jungae ^{[1
]}

Ham, Jungyeob ^{[2
]}

Kang, Heonjoong ^{[1
,3
]}

机构：

[1] Seoul Natl Univ, Sch Earth & Environm Sci, Ctr Marine Nat Prod & Drug Discovery, Seoul 151747, South Korea

[2] Korea Inst Sci & Technol, Kangnung 210340, South Korea

[3] SNU, Res Inst Oceanog, Seoul 151741, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 24期

关键词：

PPAR delta-selective ligand; Anti-atherogenic agents; Intestinal polyp formation; PPAR-DELTA; MOLECULAR MODIFICATION; ATHEROSCLEROSIS; CHOLESTEROL; SULFIDES; BIOISOSTERISM; BETA/DELTA; MODELS; HEART; MICE;

D O I：

10.1016/j.bmcl.2010.10.103

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis and in vivo activity of a novel anti-atherogenic agent, isosteric selenium PPAR delta-selective ligand. This ligand did not cause significant body or liver weight changes and did not have obvious adverse effects on intestinal polyp formation. Our overall results clearly demonstrate that PPAR delta is a viable drug candidate for targeting and treating atherosclerosis. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7239 / 7242

页数：4

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