Expeditious synthesis and biological evaluation of new C-6 1,2,3-triazole adenosine derivatives A1 receptor antagonists or agonists

Org Biomol Chem. 2010 Sep 7;8(17):3874-81. doi: 10.1039/c0ob00017e. Epub 2010 Jul 9.

Abstract

The synthesis of new C-6 1,2,3-triazole adenosine derivatives via microwave assisted 1,3-dipolar cycloaddition as key step is described. The binding on membranes of cells that over express A(1) adenosine receptors (A(1)AR) was also evaluated. Among them, four compounds increased cAMP production, in a dose-dependent manner acting as antagonists of the A(1)AR, while two compounds act as agonists.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / chemical synthesis*
  • Adenosine / pharmacology
  • Animals
  • Cell Line
  • Cyclic AMP / biosynthesis
  • Humans
  • Molecular Structure
  • Purinergic P1 Receptor Agonists / chemical synthesis*
  • Purinergic P1 Receptor Agonists / pharmacology
  • Purinergic P1 Receptor Antagonists / chemical synthesis*
  • Purinergic P1 Receptor Antagonists / pharmacology
  • Receptors, Purinergic P1 / metabolism*
  • Triazoles / chemistry*

Substances

  • Purinergic P1 Receptor Agonists
  • Purinergic P1 Receptor Antagonists
  • Receptors, Purinergic P1
  • Triazoles
  • Cyclic AMP
  • Adenosine