Discovery and optimization of a series of liver X receptor antagonists
2012
Jiao, XianYun | Kopecky, David J. | Fisher, Ben | Piper, Derek E. | Labelle, Marc | McKendry, Sharon | Harrison, Martin | Jones, Stuart | Jaen, Juan | Shiau, Andrew K. | Escaron, Patrick | Danao, Jean | Chai, Anne | Coward, Peter | Kayser, Frank
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.
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