2-(2-Furanyl)-7-phenyl [1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine analogs: Highly potent, orally active, adenosine A 2A antagonists. Part 1

…, ME Cohen-Williams, GB Varty, DB Tulshian

文献索引：Matasi, Julius J.; Caldwell, John P.; Zhang, Hongtao; Fawzi, Ahmad; Cohen-Williams, Mary E.; Varty, Geoffrey B.; Tulshian, Deen B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3670 - 3674

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被引用次数: 19

摘要

The structure–activity relationship of this novel class of compounds based on 2-(2-furanyl)-7- phenyl [1, 2, 4]-triazolo [1, 5-c] pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A2A receptor antagonism. Several compounds displayed oral activity at 3mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile.