Synthesis of alkyne derivatives of a novel triazolopyrazine as A 2A adenosine receptor antagonists

G Yao, S Haque, L Sha, G Kumaravel, J Wang…

文献索引：Yao, Gang; Haque, Serajul; Sha, Li; Kumaravel, Gnanasambandam; Wang, Joy; Engber, Thomas M.; Whalley, Eric T.; Conlon, Patrick R.; Chang, Hexi; Kiesman, William F.; Petter, Russell C. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 511 - 515

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被引用次数: 53

摘要

A novel [1, 2, 4] triazolo [1, 5-a] pyrazine core was synthesized and coupled with terminal acetylenes. The structure–activity relationship of the alkynes from this novel template was studied for their in vitro and in vivo adenosine A2A receptor antagonism. Selected compounds from this series were shown to have potent in vitro and in vivo activities against adenosine A2A receptor. Compound 12, in particular, was found to be orally active at 3mg ...