1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.

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Travins JM, Bernotas RC, Kaufman DH, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J

1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):526-30. doi: 10.1016/j.bmcl.2009.11.099. Epub 2009 Nov 23.

PubMed ID

20006495 [ View in PubMed

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Abstract

A series of 1-(3-aryloxyaryl)benzimidazoles incorporating a sulfone substituent (6) was prepared. High affinity LXR ligands were identified (LXRbeta binding IC(50) values <10nM), 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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
TO-901317	Oxysterols receptor LXR-alpha	IC 50 (nM)	9	N/A	N/A	Details