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Bioorg Med Chem Lett. 2006 Oct 1;16(19):5231-7. Epub 2006 Jul 31.

Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.

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F. Hoffmann-La Roche Ltd., Pharmaceuticals Division, Preclinical Research, CH-4070 Basel, Switzerland.


A series of branched and unbranched anilinohexafluoroisopropanols related to the known sulfonamide T0901317 were prepared and evaluated as activators/modulators of both LXRalpha and LXRbeta. A structure-activity relationship was established and compounds with high potency on both the receptors were identified. Many compounds showed a tendency toward selectivity for LXRbeta versus LXRalpha. Several analogues were evaluated for effects on plasma lipoprotein levels in mice. A few of these significantly raised HDL-cholesterol levels in plasma but showed markedly different effects on liver triglyceride content, suggesting that this series may yield candidates with improved efficacy/safety profiles compared to existing molecules.

[Indexed for MEDLINE]

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