- 2-Mercaptoimidazoles, a new class of potent CCR2 antagonists.
2-Mercaptoimidazoles, a new class of potent CCR2 antagonists.
Bioorganic & medicinal chemistry letters (2005-02-26)
Guy Van Lomen, Julien Doyon, Erwin Coesemans, Staf Boeckx, Marina Cools, Mieke Buntinx, Bart Hermans, Jean Van Wauwe
PMID15729771
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.
MATERIALS