Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists

被引：28

作者：

Luckhurst, Christopher A. ^{[1
]}

Stein, Linda A. ^{[1
]}

Furber, Mark ^{[1
]}

Webb, Nicola ^{[1
]}

Ratcliffe, Marianne J. ^{[2
]}

Allenby, Gary ^{[2
]}

Botterell, Sara ^{[2
]}

Tomlinson, Wendy ^{[2
]}

Martin, Barrie ^{[1
]}

Walding, Andrew ^{[2
]}

机构：

[1] AstraZeneca R&D Charnwood, Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Discovery Biosci, Loughborough LE11 5RH, Leics, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 01期

关键词：

PPAR delta agonism; Isoindolines; Tetrahydroisoquinolines; 3,4,5-TRISUBSTITUTED ISOXAZOLES; DESIGN; ACIDS;

D O I：

10.1016/j.bmcl.2010.10.117

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor delta (PPAR delta. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation, with upregulation of pyruvate dehydrogenase kinase, isozyme 4 (PDK4) in human primary myotubes. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：492 / 496

页数：5

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