Novel diamino derivatives of [1, 2, 4] triazolo [1, 5-a][1, 3, 5] triazine as potent and selective adenosine A2A receptor antagonists

…, D Phadke, T Engber, C Huang, J Reilly…

文献索引：Vu, Chi B.; Pan, Deborah; Peng, Bo; Kumaravel, Gnanasambandam; Smits, Glenn; Jin, Xiaowei; Phadke, Deepali; Engber, Thomas; Huang, Carol; Reilly, Jennifer; Tam, Stacy; Grant, Donna; Hetu, Gregg; Petter, Russell C. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2009 - 2018

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被引用次数: 48

摘要

Piperazine derivatives of 2-furanyl [1, 2, 4] triazolo [1, 5-a][1, 3, 5] triazine have recently been demonstrated to be potent and selective adenosine A2a receptor antagonists with oral activity in rodent models of Parkinson's disease. We have replaced the piperazinyl group with a variety of linear, monocyclic, and bicyclic diamines. Of these diamines,(R)-2- (aminomethyl) pyrrolidine is a particularly potent and selective replacement for the ...