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Diaryl substituted pyrazoles as potent CCR2 receptor antagonists
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
Institution:Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. apinkerton@kalypsys.com
Abstract: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).
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