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Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists

2007; Elsevier BV; Volume: 18; Issue: 2 Linguagem: Inglês

10.1016/j.bmcl.2007.11.060

1464-3405

An‐Rong Li, Michael G. Johnson, Jiwen Liu, Xiaoqi Chen, Xiaohui Du, Jeffrey T. Mihalic, Jeffrey Deignan, Darin J. Gustin, Jason Duquette, Zice Fu, Liusheng Zhu, Andrew P. Marcus, Phillipe Bergeron, Lawrence R. McGee, Jay Danao, Bryan D. Lemon, Teresa Carabeo, Timothy J. Sullivan, Ji Ma, Liang Tang, George Tonn, Tassie L. Collins, Julio C. Medina,

Immunotherapy and Immune Responses

A series of six-six and six-five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [(125)I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of several top compounds have also been studied. This effort led to the discovery of compounds with increased potency and improved pharmacokinetic properties that could serve as useful tools to study the role of the CXCR3 receptor in vivo.