2-Aryladenine derivatives as a potent scaffold for A(1), A(3) and dual A(1)/A(3) adenosine receptor antagonists: Synthesis and structure-activity relationships

Areias Filipe; Correia Carla; Rocha AshlyBrea JoseCastro MarianLoza Maria IFernanda Proenca M.Alice Carvalho M.

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2-Aryladenine derivatives as a potent scaffold for A(1), A(3) and dual A(1)/A(3) adenosine receptor antagonists: Synthesis and structure-activity relationships

机译：2-Aryladenine derivatives as a potent scaffold for A(1), A(3) and dual A(1)/A(3) adenosine receptor antagonists: Synthesis and structure-activity relationships

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From a collection containing more than 1500 academic compounds, in silico screening identified a hit for the human A(1) adenosine receptor containing a new purine scaffold. To study the structure activity relationships of this new chemical series for adenosine receptors, a library of 24 purines was synthesized and tested in radioligand binding assays at human A(1), A(2A), A(2B) and A(3) adenosine receptor subtypes. Fourteen molecules showed potent antagonism at A(1), A(3) or dual A(1)/A(3) adenosine receptors. This purine scaffold is an important source for novel biochemical tools and/or therapeutic drugs.

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来源
《Bioorganic and medicinal chemistry》 |2019年第16期|3551-3558|共8页
作者
Areias Filipe; Correia Carla; Rocha AshlyBrea JoseCastro MarianLoza Maria IFernanda Proenca M.Alice Carvalho M.;
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作者单位

Univ Minho, Ctr Chem, Campus Gualtar, P-4710057 Braga, Portugal;

Univ Santiago de Compostela, Dept Pharmacol, Edificio CIMUS,Avda Barcelona, Santiago De Compostela;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Adenine derivatives; Adenosine receptor antagonists; 2-Arylpurine derivatives;

2-Aryladenine derivatives as a potent scaffold for A(1), A(3) and dual A(1)/A(3) adenosine receptor antagonists: Synthesis and structure-activity relationships

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