Abstract
We describe the synthesis and SAR of a new class of CCR2 antagonists based on a 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC50 values in the MCP-1 induced Ca-flux below 0.01 μM. © 2004 Elsevier Ltd. All rights reserved.
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Van Lommen, G., Doyon, J., Coesemans, E., Boeckx, S., Cools, M., Buntinx, M., … VanWauwe, J. (2005). 2-Mercaptoimidazoles, a new class of potent CCR2 antagonists. Bioorganic and Medicinal Chemistry Letters, 15(3), 497–500. https://doi.org/10.1016/j.bmcl.2004.11.064
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