Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure-activity profile

被引：18

作者：

Cacciari, Barbara ^{[3
]}

Bolcato, Chiara ^{[1
]}

Spalluto, Giampiero ^{[1
]}

Klotz, Karl-Norbet ^{[4
]}

Bacilieri, Magdalena ^{[2
]}

Deflorian, Francesca ^{[2
]}

Moro, Stefano ^{[2
]}

机构：

[1] Univ Trieste, Dipartimento Sci Farmaceut, I-34127 Trieste, Italy

[2] Univ Padua, Dipartimento Sci Farmaceut, Mol Modeling Sect, I-35131 Padua, Italy

[3] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[4] Univ Wurzburg, Inst Pharmakol & Toxikol, D-97078 Wurzburg, Germany

来源：

PURINERGIC SIGNALLING | 2007年 / 3卷 / 03期

关键词：

adenosine receptors; antagonists; binding; molecular modeling; pyrazolo-triazolo-pyrimidines;

D O I：

10.1007/s11302-006-9027-x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In the last 5 years, many efforts have been conducted searching potent and selective human A(3) adenosine antagonists. In this field several different classes of compounds, possessing very good affinity (nM range) and with a broad range of selectivity, have been proposed. Recently, our group synthesized a new series of pyrazolo-triazolo-pyrimidines bearing different substitutions at the N-5 and N-8 positions, which have been described as highly potent and selective human A(3) adenosine receptor antagonists. The present review summarizes available data and provides an overview of the structure-activity relationships found for this class of human A(3) adenosine receptor antagonists.

引用

页码：183 / 193

页数：11

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