鉴定二芳基砜类化合物为游离脂肪酸受体 4（FFA4/GPR120）的激动剂。
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
机构信息
Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
出版信息
Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. doi: 10.1016/j.bmcl.2014.05.012. Epub 2014 May 16.
PMID:24881566
Abstract
The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
摘要
本文描述了一系列二芳基磺酰胺类游离脂肪酸受体 4（FFA4/GPR120）激动剂的研究。这项工作导致了选择性 FFA4 激动剂 8（GSK137647A）和选择性 FFA4 拮抗剂 39 的发现。本文介绍了化合物 8 和 39 的体外特性。
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