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Imidazo-pyrazine derivatives as potent CXCR3 antagonists |
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| Authors: | Xiaohui Du 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 |
| Institution: | Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA |
| 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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