Discovery of Phenyl Acetic Acid Substituted Quinolines as Novel Liver X Receptor Agonists for the Treatment of Atherosclerosis
Journal of Medicinal Chemistry2006Vol. 49(21), pp. 6151–6154
Citations Over TimeTop 10% of 2006 papers
Baihua Hu, Michael D. Collini, Rayomand J. Unwalla, Christopher P. Miller, Robert R. Singhaus, Elaine Quinet, Dawn Savio, Anita Halpern, Michael Basso, James C. Keith, Valérie Clerin, Liang Chen, Christine Resmini, Qiang-Yuan Liu, Irene Feingold, Christine Huselton, Farooq Azam, Mathias Färnegårdh, Cristofer Enroth, Tomas Bonn, Annika Goos‐Nilsson, Anna Wilhelmsson, Ponnal Nambi, Jay Wrobel
Abstract
A structure-based approach was used to optimize our new class of quinoline LXR modulators leading to phenyl acetic acid substituted quinolines 15 and 16. Both compounds displayed good binding affinity for LXRbeta and LXRalpha and were potent activators in LBD transactivation assays. The compounds also increased expression of ABCA1 and stimulated cholesterol efflux in THP-1 cells. Quinoline 16 showed good oral bioavailability and in vivo efficacy in a LDLr knockout mouse model for lesions.
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