Author/Authors :
Baihua Hu، نويسنده , , James Jetter، نويسنده , , David Kaufman، نويسنده , , Robert Singhaus، نويسنده , , Ronald Bernotas، نويسنده , , Rayomand Unwalla، نويسنده , , Elaine Quinet، نويسنده , , Dawn Savio، نويسنده , , Anita Halpern، نويسنده , , Michael Basso، نويسنده , , James Keith، نويسنده , , Valerie Clerin، نويسنده , , Liang Chen، نويسنده , , Qiang-Yuan Liu، نويسنده , , Irene Feingold، نويسنده , , Christine Huselton، نويسنده , , Farooq Azam and Sylvie Recous ، نويسنده , , Annika Goos-Nilsson، نويسنده , , Anna Wilhelmsson، نويسنده , , Ponnal Nambi، نويسنده , , et al.، نويسنده ,
Abstract :
A series of phenyl acetic acid based quinolines was prepared as LXR modulators. An SAR study in which the C-3 and C-8 positions of the quinoline core were varied led to the identification of two potent LXR agonists 23 and 27. Both compounds displayed good binding affinity for LXRβ and LXRα, and increased expression of ABCA1 in THP-1 cells. These two compounds also had desirable pharmacokinetic profiles in mice and displayed in vivo efficacy in a 12-week Apo E knockout mouse lesion model.
Keywords :
Liver X receptor (LXR) , Phenyl acetic acid , LXR agonists , Quinoline
