4.5 Article

Diaryl substituted pyrazoles as potent CCR2 receptor antagonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 3, Pages 807-813

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.060

Keywords

chemokines; CCR2; MCP-1; GPCR

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We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2. Structure-activity relationship studies directed toward improving the potency led to the discovery of 23 (IC50 = 6 nM). (c) 2006 Elsevier Ltd. All rights reserved.

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