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Bioorg Med Chem Lett. 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.

Author information

1
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. xdu@amgen.com

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.

PMID:
19631529
DOI:
10.1016/j.bmcl.2009.07.021
[Indexed for MEDLINE]

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