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ID: ALA1143782

Journal: Bioorg Med Chem Lett

Title: Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists.

Authors: Zhou C, Guo L, Parsons WH, Mills SG, MacCoss M, Vicario PP, Zweerink H, Cascieri MA, Springer MS, Yang L.

Abstract: A series of racemic and homochiral alpha-aminothiazole-gamma-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.

CiteXplore: 17092717

DOI: 10.1016/j.bmcl.2006.10.059