Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370135 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
A series of biarylsulfonamides was identified as hCCR2 receptor antagonist but suffered from high plasma protein binding resulting in a >100 fold shift in activity in a functional GTPγS assay run in tandem in the presence and absence of human serum albumin. Introduction of an aryl amide with ethylenediamine linker led to compounds with reduced shifts and improved activity in whole blood.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Gren Z. Wang, Pamela A. Haile, Tom Daniel, Benjamin Belot, Andrew Q. Viet, Krista B. Goodman, Deyou Sha, Sarah E. Dowdell, Norbert Varga, Xuan Hong, Subhas Chakravorty, Christine Webb, Carla Cornejo, Alan Olzinski, Roberta Bernard, Christopher Evans,