2-芳基-3-氨甲基喹啉的合成及构效关系研究：作为胆汁酸受体 TGR5 的激动剂。
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
机构信息
Department of Chemistry, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21. doi: 10.1016/j.bmcl.2010.08.014. Epub 2010 Aug 10.
PMID:20801037
Abstract
Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes.
摘要
高通量筛选的一个苗头化合物的优化导致了 TGR5 激动剂 32 的发现，该化合物在糖尿病的啮齿动物模型中显示出活性。
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