Generic placeholder image

Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

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

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

Volume 8, Issue 26, 2002

Page: [2299 - 2332] Pages: 34

DOI: 10.2174/1381612023392838

Price: $65


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.

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

Rights & Permissions Print Export Cite as
© 2024 Bentham Science Publishers | Privacy Policy