90085-61-3Relevant articles and documents
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties
Richter, Hans G.F.,Benson,Bleicher,Blum,Chaput,Clemann,Feng,Gardes,Grether,Hartman,Kuhn,Martin,Plancher,Rudolph,Schuler,Taylor
scheme or table, p. 1134 - 1140 (2011/04/16)
Structure-guided lead optimization of recently described benzimidazolyl acetamides addressed the key liabilities of the previous lead compound 1. These efforts culminated in the discovery of 4-{(S)-2-[2-(4-chloro-phenyl)-5,6- difluoro-benzoimidazol-1-yl]-2-cyclohexyl-acetylamino}-3-fluoro-benzoic acid 7g, a highly potent and selective FXR agonist with excellent physicochemical and ADME properties and potent lipid lowering activity after oral administration to LDL receptor deficient mice.