Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists |
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| Authors: | Bongartz Jean-Pierre Buntinx Mieke Coesemans Erwin Hermans Bart Lommen Guy Van Wauwe Jean Van |
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| Institution: | Johnson & Johnson PRD, RED EU, Turnhoutseweg 30, B-2340 Beerse, Belgium. jbongart@its.inj.com |
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| Abstract: | 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. |
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