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In an attempt to molecularly design liver X receptor (LXR) beta-selective agonists, we discovered that the combination of the 2-oxochromene moiety (head) and the imidazoline-2,4-dione moiety (tail) plays an important role in the expression potency and selectivity toward LXRbeta. We synthesized a series of 2-oxochromene derivatives and identified 43 as a LXRbeta-selective agonist that increased the HDL-C level without significantly elevating the TG level and resulted in a decreased lipid-accumulation area in the aortic arch in a high-fat-and-cholesterol-fed Bio F1B hamster. In this manuscript, we report the design, synthesis and pharmacology of these 2-oxochromene derivatives.
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Reference：
Oxazolidine – Wikipedia,
Oxazolidine | C3H799NO – PubChem