Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?

Title: Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?

Volume: 8 Issue: 26

Author(s): Pier Giovanni Baraldi, Barbara Cacciari, Pier Andrea Borea, Katia Varani, Giorgia Pastorin, Tatiana Da Ros, Mojgan Aghazadeh Tabrizi, Francesca Fruttarolo and Giampiero Spalluto

Affiliation:

Keywords: pyrazolo-triazolo-pyrimidine, adenosine receptor, adenosine antagonist, adenosine receptor subtype

Abstract: Adenosine, a widely distributed modulator, regulates many physiological functions through specific cell membrane G-protein-coupled receptors classified as A1, A2A, A2B and A3. An intense medicinal chemistry effort made over the last 20 years has led to a variety of selective adenosine receptor agonists and antagonists. In particular, the pyrazolo-triazolo-pyrimidine nucleus has been strongly investigated in the last years by our group. All the modifications performed and a tentative of structure-activity-relationship is reported. In fact, the combination of different substitutions at the N7, N8 and N5 positions afford compounds which showed good affinity and selectivity for the different adenosine receptor subtypes. The data herein summarized, permit to speculate on the use of this nucleus as possible template for the adenosine receptor subtypes.

Cite this article as:

Baraldi Giovanni Pier, Cacciari Barbara, Borea Andrea Pier, Varani Katia, Pastorin Giorgia, Da Ros Tatiana, Tabrizi Aghazadeh Mojgan, Fruttarolo Francesca and Spalluto Giampiero, Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?, Current Pharmaceutical Design 2002; 8 (26) . https://dx.doi.org/10.2174/1381612023392838