Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375344 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A series of 1-(3-aryloxyaryl)benzimidazoles incorporating a sulfone substituent (6) was prepared. High affinity LXR ligands were identified (LXRβ binding IC50 values <10 nM), some with excellent agonist potency and efficacy in a functional assay of LXR activity measuring ABCA1 mRNA increases in human macrophage THP1 cells. The compounds were typically stable in liver microsome preparations and had good oral exposure in mice.
Graphical abstractReplacement of a quinoline with a benzimidazole provided a series of liver X receptor agonists (6).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeremy M. Travins, Ronald C. Bernotas, David H. Kaufman, Elaine Quinet, Ponnal Nambi, Irene Feingold, Christine Huselton, Anna Wilhelmsson, Annika Goos-Nilsson, Jay Wrobel,