Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5891-4. doi: 10.1016/j.bmcl.2010.07.095. Epub 2010 Aug 1.

Abstract

Potent and selective adenosine A(1) receptor antagonists were disclosed. SAR and pharmacological profile of selected compounds were discussed.

MeSH terms

  • Adenosine A1 Receptor Antagonists / chemical synthesis
  • Adenosine A1 Receptor Antagonists / chemistry*
  • Adenosine A1 Receptor Antagonists / pharmacokinetics
  • Animals
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Receptor, Adenosine A1 / chemistry*
  • Receptor, Adenosine A1 / metabolism
  • Structure-Activity Relationship

Substances

  • Adenosine A1 Receptor Antagonists
  • Pyrazoles
  • Receptor, Adenosine A1