Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372206 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Potent sulfone-containing di- and trisubstituted cyclohexanes were synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the trisubstituted derivative 54, which exhibited excellent binding (CCR2 IC50 = 1.3 nM) and functional antagonism (calcium flux IC50 = 0.5 nM and chemotaxis IC50 = 0.2 nM). The superiority of the trisubstituted scaffold was rationalized to be the result of a conformational rigidification, which provided insight into the bioactive conformation of this chemotype.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert J. Cherney, Ruowei Mo, Dayton T. Meyer, Matthew E. Voss, Yvonne C. Lo, Gengjie Yang, Persymphonie B. Miller, Peggy A. Scherle, Andrew J. Tebben, Percy H. Carter, Carl P. Decicco,