279682-93-8Relevant 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 (2007/10/03)
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.
Detritylation with ytterbium triflate
Lu, Rong Jian,Liu, Daipei,Giese, Roger W.
, p. 2817 - 2819 (2007/10/03)
Ytterbium triflate catalyzes the hydrolysis of tritylamines and trityloxy compounds to the corresponding amines and alcohols under mild conditions in high yields. The reactions are conducted in tetrahydrofuran in the presence of 1 equivalent of water. (C) 2000 Elsevier Science Ltd.
