2-(2-Furanyl)-7-phenyl [1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine analogs as adenosine A 2A antagonists: The successful reduction of hERG activity. Part 2

…, A Fawzi, GA Higgins, ME Cohen-Williams…

文献索引：Matasi, Julius J.; Caldwell, John P.; Zhang, Hongtao; Fawzi, Ahmad; Higgins, Guy A.; Cohen-Williams, Mary E.; Varty, Geoffrey B.; Tulshian, Deen B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3675 - 3678

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被引用次数: 23

摘要

The structure–activity relationship (SAR) exploration using 2-(2-furanyl)-7-phenyl [1, 2, 4] triazolo-[1, 5-c] pyrimidin-5-amine (1) as a template led to the identification of a novel class of potent and selective adenosine A2A receptor (AR) antagonists. However, these compounds were found to be associated with significant hERG activity. This report discusses the strategy and outcome of an expanded SAR focused on addressing the hERG liability. ...