3-(3-芳氧基苯基)咪唑并[1,2-a]吡啶砜类作为肝 X 受体激动剂。
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
机构信息
Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):521-5. doi: 10.1016/j.bmcl.2009.11.098. Epub 2009 Nov 23.
PMID:20005711
Abstract
Replacement of a quinoline with an imidazo[1,2-a]pyridine in a series of liver X receptor (LXR) agonists incorporating a [3-(sulfonyl)aryloxyphenyl] side chain provided high affinity LXR ligands 7. In functional assays of LXR activity, good agonist potency and efficacy were found for several analogs.
摘要
在一系列包含[3-(磺酰基)芳氧基苯基]侧链的肝 X 受体 (LXR) 激动剂中，用咪唑并[1,2-a]吡啶取代喹啉，得到了高亲和力的 LXR 配体 7。在 LXR 活性的功能测定中，发现几种类似物具有良好的激动剂效力和功效。
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