3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.

Article Details

Citation

Singhaus RR, Bernotas RC, Steffan R, Matelan E, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J

3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):521-5. doi: 10.1016/j.bmcl.2009.11.098. Epub 2009 Nov 23.

PubMed ID
20005711 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TO-901317Oxysterols receptor LXR-alphaIC 50 (nM)9N/AN/ADetails
TO-901317Oxysterols receptor LXR-alphaEC 50 (nM)170N/AN/ADetails