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Bioorganic & medicinal chemistry letters

Discovery and optimization of a series of liver X receptor antagonists.


PMID 22901900

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.

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108146
Benzenesulfonamide, ≥98%
C6H7NO2S