Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375608 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of trisubstituted cyclohexanes was designed, synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the identification of two distinct substitution patterns about the cyclohexane ring as potent and selective CCR2 antagonists. Compound 36 exhibited excellent binding (CCR2 IC50 = 2.4 nM) and functional antagonism (calcium flux IC50 = 2.0 nM and chemotaxis IC50 = 5.1 nM).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert J. Cherney, John B. Brogan, Ruowei Mo, Yvonne C. Lo, Gengjie Yang, Persymphonie B. Miller, Peggy A. Scherle, Bruce F. Molino, Percy H. Carter, Carl P. Decicco,