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

  • Bioorg Med Chem Lett. 2008 Nov 1;18(21):5819-23. doi: 10.1016/j.bmcl.2008.07.115.
Jean-Pierre Bongartz  1 ,  Mieke Buntinx ,  Erwin Coesemans ,  Bart Hermans ,  Guy Van Lommen ,  Jean Van Wauwe
Affiliations
  • 1. Johnson & Johnson PRD, RED EU, Turnhoutseweg 30, B-2340 Beerse, Belgium. [email protected]
PMID: 18922694 DOI: 10.1016/j.bmcl.2008.07.115
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.