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.
Robert R Singhaus  1 ,  Ronald C Bernotas ,  Robert Steffan ,  Edward Matelan ,  Elaine Quinet ,  Ponnal Nambi ,  Irene Feingold ,  Christine Huselton ,  Anna Wilhelmsson ,  Annika Goos-Nilsson ,  Jay Wrobel
Affiliations
  • 1. Chemical Sciences, Wyeth Pharmaceuticals, 500 Arcola Rd., Collegeville, PA 19426, USA. [email protected]
PMID: 20005711 DOI: 10.1016/j.bmcl.2009.11.098
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.