- Discovery and optimization of a series of liver X receptor antagonists.
Discovery and optimization of a series of liver X receptor antagonists.
Bioorganic & medicinal chemistry letters (2012-08-21)
XianYun Jiao, David J Kopecky, Ben Fisher, Derek E Piper, Marc Labelle, Sharon McKendry, Martin Harrison, Stuart Jones, Juan Jaen, Andrew K Shiau, Patrick Escaron, Jean Danao, Anne Chai, Peter Coward, Frank Kayser
PMID22901900
ABSTRACT
The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was determined to be potent dual liver X receptor (LXR α/β) ligands. Herein we report the identification of compound 54 as the first reported LXR antagonist that is suitable for pharmacological in vivo evaluation in rodents.
MATERIALS