Synthesis of alkyne derivatives of a novel triazolopyrazine as A<sub>2Asub> adenosine receptor antagonists

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• 作者：Yao ; Gang ; Haque ; Serajul ; Sha ; Li ; Kumaravel ; Gnanasambandam ; Wang ; Joy ; Engber ; Thomas M. ; et. al.
• 关键词：A<sub>2Asub> antagonists ; Parkinson脙脙脙脙脙脙s disease ; Triazolopyrazine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：February 1, 2005
• 卷：15
• 期：3
• 页码：511-515
• 文件大小：129 K

摘要

A novel [1,2,4]triazolo[1,5-a]pyrazine core was synthesized and coupled with terminal acetylenes. The structure芒芒芒activity relationship of the alkynes from this novel template was studied for their in vitro and in vivo adenosine A<sub>2Asub> receptor antagonism. Selected compounds from this series were shown to have potent in vitro and in vivo activities against adenosine A<sub>2Asub> receptor. Compound 12, in particular, was found to be orally active at 3mg/kg in both a mouse catalepsy model and a 6-hydroxydopamine-lesioned rat model.