Diaryl substituted pyrazoles as potent CCR2 receptor antagonists

We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2b. Structure–activity relationship studies directed toward improving the potency led to the discovery of 23 (IC 50 = 6 nM). We have identified and synthesized a series...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (3), p.807-813
Main Authors: Pinkerton, Anthony B., Huang, Dehua, Cube, Rowena V., Hutchinson, John H., Struthers, Mary, Ayala, Julia M., Vicario, Pasquale P., Patel, Sima R., Wisniewski, Thomas, DeMartino, Julie A., Vernier, Jean-Michel
Format: Article
Language:English
Subjects:
Biological and medical sciences
CCR2
Chemokines
Chemotaxis - drug effects
GPCR
Humans
In Vitro Techniques
Indicators and Reagents
MCP-1
Medical sciences
Miscellaneous
Monocytes - drug effects
Oxidation-Reduction
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Receptors, CCR2
Receptors, Chemokine - antagonists & inhibitors
Receptors, Chemokine - drug effects
Structure-Activity Relationship
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Summary:We have identified and synthesized a series of diaryl substituted pyrazoles as potent antagonists of the chemokine receptor subtype 2b. Structure–activity relationship studies directed toward improving the potency led to the discovery of 23 (IC 50 = 6 nM). 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 (IC 50 = 6 nM).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.10.060