Studies towards the conception of new selective PPARβ/δ ligands

被引：17
|
作者：
Ekambome Bassene, Carine
Suzenet, Franck
Hennuyer, Nathalie
Staels, Bart
Caignard, Daniel-Henri
Dacquet, Catherine
Renard, Pierre
Guillaumet, Gerald
机构：
[1] Univ Orleans, CNRS, UMR 6005, ICOA,FR 2708, F-45067 Orleans 02, France
[2] Inst Pasteur, U545, Dept Atherosclerose, F-59019 Lille, France
[3] Inst Rech Servier, Etut Exterieures & Alliance Strateg, F-78390 Croissy Sur Seine, France
[4] Inst Rech Servier, Div Malad Metab, F-92150 Suresnes, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 17期
关键词：
nuclear receptor; PPAR beta/delta; pyridine;
D O I：
10.1016/j.bmcl.2006.06.028
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In order to define new PPAR beta/delta ligands, SAR study on the selective PPAR beta/delta activator L-165,041 led to the identification of one key functional group for selective PPAR beta/delta activation. Further-more, taking advantage of SAR studies done elsewhere on the most selective PPAR beta/delta ligand GW501516, the conception of new ligands showing good affinity for PPAR beta/delta is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPAR beta/ delta subtype selectivity. (c) 2006 Published by Elsevier Ltd.
引用
收藏
页码：4528 / 4532
页数：5
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