fexaramine and Non-alcoholic-Fatty-Liver-Disease

A series of fexaramine analogs were synthesized and evaluated to develop an intestine-selective/specific FXR partial agonist. Introduction of both a CN substituent at the C-2 in the biphenyl ring and a fluorine at the C-5 in the aniline ring in fexaramine markedly increased FXR agonistic activity.

Topics: Acrylates; Animals; Bile Acids and Salts; Esters; Intestines; Liver; Mice; Non-alcoholic Fatty Liver Disease; Rats; Receptors, Cytoplasmic and Nuclear