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

Article abstract of DOI:10.1016/j.bmcl.2008.07.115

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.