Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides

Bioorg Med Chem Lett. 2009 May 15;19(10):2664-7. doi: 10.1016/j.bmcl.2009.03.142. Epub 2009 Apr 1.

Abstract

A novel series of antagonists of the human A(2A) receptor have been identified and have been shown to display good potency and high degrees of selectivity over other receptor sub-types. Displaying in vivo potency in commonly used disease models and high oral bio-availability, this class of compounds may serve as clinically useful treatments for the relief of the symptoms associated with Parkinson's disease.

MeSH terms

  • Adenosine A2 Receptor Antagonists*
  • Administration, Oral
  • Amides / administration & dosage
  • Amides / chemical synthesis*
  • Amides / chemistry
  • Animals
  • Disease Models, Animal
  • Humans
  • Mice
  • Pyrimidines / chemistry*
  • Receptor, Adenosine A2A / metabolism

Substances

  • Adenosine A2 Receptor Antagonists
  • Amides
  • Pyrimidines
  • Receptor, Adenosine A2A