8-Benzylaminoxanthine scaffold variations for selective ligands acting on adenosine A 2A receptors. Design, synthesis and biological evaluation.

Michał Załuski, Jakub Schabikowski, Piotr Jaśko,Adrian Bryła,Agnieszka Olejarz-Maciej,Maria Kaleta,Monika Głuch-Lutwin,Andreas Brockmann,Sonja Hinz,Małgorzata Zygmunt,Kamil Kuder,Gniewomir Latacz,Christin Vielmuth,Christa E Müller,Katarzyna Kieć-Kononowicz

Bioorganic Chemistry（2020）

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摘要

•Novel library of 8-benzylaminoxanthine derivatives was designed and synthesized.•Potent and selective ligands of A2A or (A1,A2A) adenosine receptors were found.•SAR for the synthesized series supported by molecular docking was analyzed.•Metabolic stability of most active A2A ligand was evaluated in silico and in vitro.•Preliminary in vivo anti-inflammatory tests were performed for most promising ligand.

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关键词

Adenosine A2Areceptors,Anti-inflammatory activity,Metabolic stability,Molecular docking,Monoamine oxidase,Phosphodiesterase,Xanthine derivatives

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