Discovery of aminoquinazoline derivatives as human A_2A adenosine receptor antagonists

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• 作者：Gang Zhou^a ; ; Robert Aslanian^b ; Gioconda Gallo^a ; Tanweer Khan^b ; Rongze Kuang^a ; Biju Purakkattle^b ; Manuel De Ruiz^c ; Andrew Stamford^a ; Pauline Ting^a ; Heping Wu^a ; Hongwu Wang^b ; Dong Xiao^b ; Tao Yu^a ; Yonglian Zhang^a ; Deborra Mullins^b ; Robert Hodgson^b
• 关键词：Adenosine A2A receptor antagonist ; Aminoquinazoline ; Parkinson&rsquo ; s disease
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：26
• 期：4
• 页码：1348-1354
• 全文大小：4318 K

文摘

Novel bicyclic adenosine A_2A antagonists with an aminoquinazoline moiety were designed and synthesized. The optimization of the initial lead compound based on in vitro and in vivo activity has led to the discovery of a potent and selective class of adenosine A_2A antagonists. The structure–activity relationships of this novel series of bicyclic aminoquinazoline derivatives as adenosine A_2A antagonists are described in detail.