Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes

被引：108

作者：

Christiansen, Elisabeth ^{[1
]}

Urban, Christian ^{[2
]}

Merten, Nicole ^{[3
]}

Liebscher, Kathrin ^{[4
]}

Karlsen, Kasper K. ^{[1
]}

Hamacher, Alexandra ^{[2
]}

Spinrath, Andreas ^{[3
]}

Bond, Andrew D. ^{[1
]}

Drewke, Christel ^{[3
]}

Ullrich, Susanne ^{[4
]}

Kassack, Matthias U. ^{[2
]}

Kostenis, Evi ^{[3
]}

Ulven, Trond ^{[1
]}

机构：

[1] Univ So Denmark, Dept Chem & Phys, DK-5230 Odense M, Denmark

[2] Univ Dusseldorf, Inst Pharmaceut & Med Chem, D-40225 Dusseldorf, Germany

[3] Univ Bonn, Inst Pharmaceut Biol, Dept Mol Cellular & Pharmacobiol, D-53115 Bonn, Germany

[4] Univ Tubingen, Dept Internal Med, Div Endocrinol Diabetol Vasc Med Nephrol & Clin C, D-72076 Tubingen, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 22期

基金：

英国医学研究理事会;

关键词：

D O I：

10.1021/jm8010178

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC50 = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.

引用

页码：7061 / 7064

页数：4

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