5,7-Disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazines as pharmacological tools to explore the antagonist selectivity profiles toward adenosine receptors
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- 作者：Stephanie Federicoa ; Antonella Ciancettab ; Nicola Portab ; Sara Redentia ; Giorgia Pastorinc ; Barbara Cacciarid ; Karl Norbert Klotze ; Stefano Morob ; stefano.moro@unipd.it" class="auth_mail" title="E-mail the corresponding author ; Giampiero Spallutoa ; spalluto@units.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：G protein-coupled receptor ; Antagonists ; Molecular modeling ; Structure activity relationship ; Triazolo-triazine ; Adenosine receptors
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：529-541
- 全文大小：2279 K
文摘
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A series of triazolo-triazines was developed as adenosine receptor (AR) antagonists.
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Compounds show better affinity at the hA2A and hA3 ARs than at the hA1 and hA2B ARs.
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A benzylamino group at the C5 position gives highest affinity values at the hARs.
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Docking simulations were carried out to explain the observed binding data.