Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A₁ receptor antagonists

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• 作者：Georgios Alachouzos ; Eelke B. Lenselink ; Thea Mulder-Krieger ; Henk de Vries ; Adriaan P. IJzerman ; Julien Louvelp> ; p>p>j.a.louvel@lacdr.leidenuniv.nlp>
• 关键词：Structure-affinity relationships ; Adenosine A1 receptor ; Adenosine A2A receptor ; Selectivity ; Antagonists
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：586-602
• 全文大小：1104 K
• 卷排序：125

文摘

51 2-amino-4,5-diarylpyrimidines synthesized. Affinity and functional data reported at hA1 and hA2A adenosine receptor. Introduction of N2-substituents, great increase in hA1 selectivity. Docking studies in ligand-optimized (homology) models to rationalize selectivity.