Author/Authors :
Guy Van Lommen، نويسنده , , Julien Doyon، نويسنده , , Erwin Coesemans، نويسنده , , Staf Boeckx، نويسنده , , Marina Cools، نويسنده , , Mieke Buntinx، نويسنده , , Bart Hermans، نويسنده , , Jean VanWauwe، نويسنده ,
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.