1297603-68-9Relevant articles and documents
Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes
Richter, Hans G.F.,Benson, Gregory M.,Blum, Denise,Chaput, Evelyne,Feng, Song,Gardes, Christophe,Grether, Uwe,Hartman, Peter,Kuhn, Bernd,Martin, Rainer E.,Plancher, Jean-Marc,Rudolph, Markus G.,Schuler, Franz,Taylor, Sven,Bleicher, Konrad H.
experimental part, p. 191 - 194 (2011/02/28)
Herein we describe the synthesis and structure activity relationship of a new class of FXR agonists identified from a high-throughput screening campaign. Further optimization of the original hits led to molecules that were highly active in an LDL-receptor KO model for dyslipidemia. The most promising candidate is discussed in more detail.