183732-58-3Relevant academic research and scientific papers
Discovery of 3,5-bis(trifluoromethyl)benzyl l-arylglycinamide based potent CCR2 antagonists
Yang, Lihu,Zhou, Changyou,Guo, Liangqin,Morriello, Gregori,Butora, Gabor,Pasternak, Alexander,Parsons, William H.,Mills, Sander G.,MacCoss, Malcolm,Vicario, Pasquale P.,Zweerink, Hans,Ayala, Julia M.,Goyal, Shefali,Hanlon, William A.,Cascieri, Margaret A.,Springer, Marty S.
, p. 3735 - 3739 (2006)
Systematic modification of a screening lead yielded a class of potent glycinamide based CCR2 antagonists. The best compound (55, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-{[2-(1-piperidinyl)ethyl]amino}-2-(3-thienyl)acetamide) displayed good binding affinity (IC50 = 30 and 39 nM) toward human monocytes and CHO cell expressing human CCR2b, respectively. Functionally, it blocked MCP-1 (CCL2)-induced calcium mobilization (IC50 = 50 nM) and chemotaxis mediated through the CCR2 receptor (9.6 nM). It is selective against other chemokine receptors tested.
