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Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor beta-selective agonists
A novel series of 1,3-bistrifluoromethylcarbinol derivatives that act as liver X receptor (LXR) beta-selective agonists was discovered. Structure-activity relationship studies led to the identification of molecule 62, which was more effective (Emax) and selective toward LXRbeta than T0901317 and GW3965. Furthermore, 62 decreased LDL-C without elevating the plasma TG level and significantly suppressed the lipid-accumulation area in the aortic arch in a Bio F1B hamster fed a diet high in fat and cholesterol. We demonstrated that our LXRbeta agonist would be potentially useful as a hypolipidemic and anti-atherosclerotic agent. In this manuscript, we report the design, synthesis and pharmacology of 1,3-bistrifluoromethylcarbinol derivatives.
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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem