Author/Authors :
Changyou Zhou، نويسنده , , Liangqin Guo، نويسنده , , William H. Parsons، نويسنده , , Sander G. Mills، نويسنده , , Malcolm MacCoss، نويسنده , , Pasquale P. Vicario، نويسنده , , Hans Zweerink، نويسنده , , Margaret A. Cascieri، نويسنده , , Martin S. Springer، نويسنده , , Lihu Yang، نويسنده ,
Abstract :
A series of racemic and homochiral α-aminothiazole-γ-aminobutyroamides that display high affinities for human and murine CCR2 and functional antagonism by inhibition of monocyte recruitment are described. A representative example is (2S)-2-[2-(acetylamino)-1,3-thiazol-4-yl]-N-[3-methyl-5-(trifluoromethyl)benzyl]-4-(4-phenylpiperidin-1-yl)butanamide, which shows 5 nM affinity for human monocytes and CHO cells expressing the human CCR2b receptor. It also inhibited MCP-1 initiated chemotaxis of human monocytes with an IC50 of 0.69 nM.
Keywords :
CCR2 , Antagonist , monocyte , Chemotaxis , Aminothiazole
