Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRα and β

N Panday, J Benz, D Blum-Kaelin, V Bourgeaux…

Index: Panday, Narendra; Benz, Joerg; Blum-Kaelin, Denise; Bourgeaux, Vanessa; Dehmlow, Henrietta; Hartman, Peter; Kuhn, Bernd; Ratni, Hassen; Warot, Xavier; Wright, Matthew B. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 19 p. 5231 - 5237

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Citation Number: 10

Abstract

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 ...