Epple Robert, Azimioara Mihai, Russo Ross, Bursulaya Badry, Tian Shin-Shay, Gerken Andrea, Iskandar Maya
Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20.
A series of highly potent and selective PPARdelta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 microM, making it a useful tool in studying the biological effects of selective PPARdelta activation.
以已知的非选择性配体GW2433为结构模板，描述了一系列高效且选择性的PPARδ激动剂。化合物1具有生物利用度，活性强（10 nM），在高达10 μM的浓度下与其他PPAR亚型无交叉活性，使其成为研究选择性PPARδ激活的生物学效应的有用工具。
