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. 2009 Sep 1;19(17):5200-4.
doi: 10.1016/j.bmcl.2009.07.021. Epub 2009 Jul 9.

Imidazo-pyrazine derivatives as potent CXCR3 antagonists

Xiaohui Du  1 , Darin J Gustin, Xiaoqi Chen, Jason Duquette, Lawrence R McGee, Zhulun Wang, Karen Ebsworth, Kirk Henne, Bryan Lemon, Ji Ma, Shichang Miao, Emmanuel Sabalan, Timothy J Sullivan, George Tonn, Tassie L Collins, Julio C Medina
Affiliations

Imidazo-pyrazine derivatives as potent CXCR3 antagonists

Xiaohui Du et al. Bioorg Med Chem Lett. .

Abstract

A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to increased potency. The efficacy of the lead compound 21 is evaluated in a mouse lung inflammation model.

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