Novel phenyl-urea derivatives as dual-target ligands that can activate both GK and PPARγ

A series of novel phenyl-urea derivatives which can simultaneously activate glucokinase (GK) and peroxisome proliferator-activated receptor γ (PPARγ) was designed and prepared, and their activation of GK and PPARγ was evaluated. The structure–activity relationships of these compounds are also described. Three compounds showed potent ability to activate both GK and PPARγ. The possible binding mode of one of these compounds with GK and PPARγ were predicted by molecular docking simulation.

Graphical abstractA series of novel phenyl-urea derivatives which can simultaneously activate GK and PPARγ was designed, prepared and evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide