Biarylether amide quinolines as liver X receptor agonists

…, A Wilhelmsson, A Goos-Nilsson, M Farnegardh…

文献索引：Bernotas, Ronald C.; Singhaus, Robert R.; Kaufman, David H.; Ullrich, John; Fletcher III, Horace; Quinet, Elaine; Nambi, Ponnal; Unwalla, Rayomand; Wilhelmsson, Anna; Goos-Nilsson, Annika; Farnegardh, Mathias; Wrobel, Jay Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 4 p. 1663 - 1670

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被引用次数: 25

摘要

A series of 4-(amido-biarylether)-quinolines was prepared as potential LXR agonists. Appropriate substitution with amide groups provided high affinity LXR ligands, some with excellent potency and efficacy in functional assays of LXR activity. Novel amide 4g had a binding IC50= 1.9 nM for LXRβ and EC50= 34nM (96% efficacy relative to T0901317) in an ABCA1 gene expression assay in mouse J774 cells, demonstrating that 4-(biarylether)- ...