One-Pot Reaction To Obtain N,N鈥?Disubstituted Guanidines of Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine Scaffold as Human A3 Adenosine Receptor Antagonists

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• 作者：Pier Giovanni Baraldi ; Stefania Baraldi ; Giulia Saponaro ; Mojgan Aghazadeh Tabrizi ; Romeo Romagnoli ; Emanuela Ruggiero ; Fabrizio Vincenzi ; Pier Andrea Borea ; Katia Varani
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：July 9, 2015
• 年：2015
• 卷：58
• 期：13
• 页码：5355-5360
• 全文大小：298K
• ISSN：1520-4804

文摘

In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A₃AR antagonist. Our initial aim was to replace the phenylcarbamoyl moiety at the 5 position of PTP nucleus with a thiourea functionality to evaluate the contribution of new structural modification against the A₃AR. The synthesized 12鈥?b>25 were not characterized by the predicted side chain but by a 1,3-disubstituted guanidine and are shown to be interesting A₃AR antagonists.