title: Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.
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).
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. apinkerton@kalypsys.com
authors.forename: Anthony B
authors.initials: AB
authors.lastname: Pinkerton
authors.forename: Dehua
authors.initials: D
authors.lastname: Huang
authors.forename: Rowena V
authors.initials: RV
authors.lastname: Cube
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: Mary
authors.initials: M
authors.lastname: Struthers
authors.forename: Julia M
authors.initials: JM
authors.lastname: Ayala
authors.forename: Pasquale P
authors.initials: PP
authors.lastname: Vicario
authors.forename: Sima R
authors.initials: SR
authors.lastname: Patel
authors.forename: Thomas
authors.initials: T
authors.lastname: Wisniewski
authors.forename: Julie A
authors.initials: JA
authors.lastname: DeMartino
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Vernier
mesh_terms: D002633:Chemotaxis / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009000:Monocytes / Q000187:drug effects; D010084:Oxidation-Reduction; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D054390:Receptors, CCR2; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors* / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: C515334:CCR2 protein, human; D007202:Indicators and Reagents; D011720:Pyrazoles; D054390:Receptors, CCR2; D019707:Receptors, Chemokine