Synthesis and structure–activity relationship of benzetimide derivatives as human CXCR3 antagonists

The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-cholinergic activity and identification of the key pharmacophore moieties of the series.

Graphical abstractA novel class of CXCR3 antagonist is explored for its key contributing moieties toward its potency and selectivity regarding unwanted anti-cholinergic activity.Figure optionsDownload full-size imageDownload as PowerPoint slide