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

…, E Coesemans, B Hermans, G Van Lommen…

文献索引：Bongartz, Jean-Pierre; Buntinx, Mieke; Coesemans, Erwin; Hermans, Bart; Lommen, Guy Van; Wauwe, Jean Van Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 21 p. 5819 - 5823

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被引用次数: 15

摘要

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.