| Literature DB >> 20346664 |
Robert J Cherney1, Ruowei Mo, Dayton T Meyer, Matthew E Voss, Michael G Yang, Joseph B Santella, John V Duncia, Yvonne C Lo, Gengjie Yang, Persymphonie B Miller, Peggy A Scherle, Qihong Zhao, Sandhya Mandlekar, Mary Ellen Cvijic, Joel C Barrish, Carl P Decicco, Percy H Carter.
Abstract
We describe the design, synthesis, and evaluation, of gamma-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 IC(50)=1.0 nM and chemotaxis IC(50) = 0.5 nM) and improved metabolic stability over its parent glycinamide. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20346664 DOI： 10.1016/j.bmcl.2010.03.035
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823