New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A 2A adenosine receptor antagonists.

Matteo Falsini,Costanza Ceni,Daniela Catarzi,Flavia Varano,Diego Dal Ben,Gabriella Marucci,Michela Buccioni,Aleix Martí Navia,Rosaria Volpini,Vittoria Colotta

Bioorganic & Medicinal Chemistry Letters（2020）

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摘要

•Synthesis of novel 8-amino-6-aryl-2-phenyl-1,2,4-triazolo[4,3-a]pyrazin-3-ones.•1,2,4-Triazolo[4,3-a]pyrazin-3-ones as potent hA2A adenosine receptor antagonists.•Docking studies of 1,2,4-triazolo[4,3-a]pyrazin-3-ones at the hA2A adenosine receptor.

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关键词

G protein-coupled receptors,A2A adenosine receptor antagonists,1,2,4-Triazolo[4,3-a]pyrazin-3-ones,Ligand-adenosine receptor modeling studies

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