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

Zhou, Changyou ; Guo, Liangqin ; Parsons, William H ; Mills, Sander G ; Maccoss, Malcolm ; Vicario, Pasquale P ; Zweerink, Hans ; Cascieri, Margaret A ; Springer, Martin S ; Yang, Lihu

Bioorganic & medicinal chemistry letters, 15 January 2007, Vol.17(2), pp.309-14 [Peer Reviewed Journal]

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  • Title:
    Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists
  • Author: Zhou, Changyou ; Guo, Liangqin ; Parsons, William H ; Mills, Sander G ; Maccoss, Malcolm ; Vicario, Pasquale P ; Zweerink, Hans ; Cascieri, Margaret A ; Springer, Martin S ; Yang, Lihu
  • Description: 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.
  • Is Part Of: Bioorganic & medicinal chemistry letters, 15 January 2007, Vol.17(2), pp.309-14
  • Identifier: ISSN: 0960-894X ; PMID: 17092717 Version:1
  • Subjects: Receptors, Chemokine -- Antagonists & Inhibitors
  • Language: English
  • Source: MEDLINE/PubMed (U.S. National Library of Medicine)

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