Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375094 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
We describe the design, synthesis, and evaluation, of γ-lactams as glycinamide replacements within a series of di- and trisubstituted cyclohexane CCR2 antagonists. The lactam-containing trisubstituted cyclohexanes proved to be more potent than the disubstituted analogs, as trisubstituted analog, lactam 13, displayed excellent activity (CCR2 binding IC50 = 1.0 nM and chemotaxis IC50 = 0.5 nM) and improved metabolic stability over its parent glycinamide.
Graphical abstractWe describe the design, synthesis, and evaluation, of γ-lactams as glycinamide replacements within a series of di- and trisubstituted cyclohexane CCR2 antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert J. Cherney, Ruowei Mo, Dayton T. Meyer, Matthew E. Voss, Michael G. Yang, Joseph B. Santella III, John V. Duncia, Yvonne C. Lo, Gengjie Yang, Persymphonie B. Miller, Peggy A. Scherle, Qihong Zhao, Sandhya Mandlekar, Mary Ellen Cvijic,