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3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists
Authors:Robert R Singhaus  Ronald C Bernotas  Robert Steffan  Edward Matelan  Elaine Quinet  Ponnal Nambi  Irene Feingold  Christine Huselton  Anna Wilhelmsson  Annika Goos-Nilsson  Jay Wrobel
Institution:1. Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA;2. Cardiovascular and Metabolic Diseases, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA;3. Drug Safety and Metabolism, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA;4. Karo Bio AB, Novum S-141, 57 Huddinge, Sweden
Abstract:Replacement of a quinoline with an imidazo1,2-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.
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