Title of article
α-Aminothiazole-γ-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
309
To page
314
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797645
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