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ID: ALA1149525
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.
Authors: Panday N, Benz J, Blum-Kaelin D, Bourgeaux V, Dehmlow H, Hartman P, Kuhn B, Ratni H, Warot X, Wright MB.
Abstract: 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.
CiteXplore: 16876993