Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides

Roger J Gillespie, Samantha J Bamford, Alex Clay, Suneel Gaur, Tim Haymes, Philip S Jackson, Allan M Jordan, Burkhard Klenke, Stefania Leonardi, Jeanette Liu, Howard L Mansell, Sean Ng, Mona Saadi, Heather Simmonite, Gemma C Stratton, Richard S Todd, Douglas S Williamson, Ian A Yule

Research output: Contribution to journalArticlepeer-review


Antagonists of the human A(2A) receptor have been reported to have potential therapeutic benefit in the alleviation of the symptoms associated with neurodegenerative movement disorders such as Parkinson's disease. As part of our efforts to discover potent and selective antagonists of this receptor, we herein describe the detailed optimization and structure-activity relationships of a series of pyrimidine-4-carboxamides. These optimized derivatives display desirable physiochemical and pharmacokinetic profiles, which have led to promising oral activity in clinically relevant models of Parkinson's disease.

Original languageEnglish
Pages (from-to)6590-605
Number of pages16
JournalBioorganic and Medicinal Chemistry
Issue number18
Publication statusPublished - 15 Sept 2009


  • Adenosine A2 Receptor Antagonists
  • Animals
  • Humans
  • Locomotion
  • Mice
  • Parkinson Disease
  • Protein Binding
  • Pyrimidines
  • Receptor, Adenosine A2A
  • Structure-Activity Relationship

Research Beacons, Institutes and Platforms

  • Manchester Cancer Research Centre


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