Imidazo-pyrazine derivatives as potent CXCR3 antagonists

…, Z Wang, K Ebsworth, K Henne, B Lemon, J Ma…

Index: Du, Xiaohui; Gustin, Darin J.; Chen, Xiaoqi; Duquette, Jason; McGee, Lawrence R.; Wang, Zhulun; Ebsworth, Karen; Henne, Kirk; Lemon, Bryan; Ma, Ji; Miao, Shichang; Sabalan, Emmanuel; Sullivan, Timothy J.; Tonn, George; Collins, Tassie L.; Medina, Julio C. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 17 p. 5200 - 5204

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Citation Number: 26

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.