2-Mercaptoimidazoles, a new class of potent CCR2 antagonists |
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| Authors: | Van Lomen Guy Doyon Julien Coesemans Erwin Boeckx Staf Cools Marina Buntinx Mieke Hermans Bart Van Wauwe Jean |
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| Institution: | Inflammation Research, Johnson and Johnson Pharmaceutical Research and Development, Beerse, Belgium. gvlommen@prdbe.jnj.com |
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| Abstract: | We describe the synthesis and SAR of a new class of CCR2 antagonists based on 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC(50) values in the MCP-1 induced Ca-flux below 0.01 microM. |
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