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Imidazo-pyrazine derivatives as potent CXCR3 antagonists

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
19
Issue
17
Identifiers
DOI: 10.1016/j.bmcl.2009.07.021
Keywords
  • Cxcr3 Antagonist
  • Imidazo-Pyrazine
Disciplines
  • Pharmacology

Abstract

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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