Imidazo[1,2-a]pyrazin-8-amine core for the design of new adenosine receptor antagonists: Structural exploration to target the A₃ and A_2A subtypes

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• 作者：Daniela Poli^a ; Matteo Falsini^a ; Flavia Varano^a ; Marco Betti^a ; Katia Varani^b ; Fabrizio Vincenzi^b ; Anna Maria Pugliese^c ; Felicita Pedata^c ; Diego Dal Ben^d ; Ajiroghene Thomas^d ; Ilaria Palchetti^e ; ^f ; Francesca Bettazzi^e ; Daniela Catarzi^a ; ^{daniela.catarzi@unifi.it} ; Vittoria Colotta^a
• 关键词：G protein-coupled receptors ; Adenosine receptor antagonists ; Imidazopyrazines ; Bicyclic heteroaromatic systems ; Ligand-receptor modeling studies
• 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：611-628
• 全文大小：1728 K
• 卷排序：125

文摘

Imidazo[1,2-a]pyrazine-8-amine core for the design of human A3 and A2A adenosine receptor antagonists. Identification of new potent and selective adenosine A3 receptor antagonists. Pharmacological evaluation in an in vitro rat model of cerebral ischemia. Fluorescence emission property determination. Molecular docking analysis at our human A3 receptor model.