1992-24-1Relevant articles and documents
Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRα and β
Panday, Narendra,Benz, Joerg,Blum-Kaelin, Denise,Bourgeaux, Vanessa,Dehmlow, Henrietta,Hartman, Peter,Kuhn, Bernd,Ratni, Hassen,Warot, Xavier,Wright, Matthew B.
, p. 5231 - 5237 (2007/10/03)
A series of branched and unbranched anilinohexafluoroisopropanols related to the known sulfonamide T0901317 were prepared and evaluated as activators/modulators of both LXRα and LXRβ. 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 LXRβ versus LXRα. 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.