Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3. doi: 10.1016/j.bmcl.2008.03.076.
Roger J Gillespie  1 ,  Ian A Cliffe ,  Claire E Dawson ,  Colin T Dourish ,  Suneel Gaur ,  Paul R Giles ,  Allan M Jordan ,  Antony R Knight ,  Anthony Lawrence ,  Joanne Lerpiniere ,  Anil Misra ,  Robert M Pratt ,  Richard S Todd ,  Rebecca Upton ,  Scott M Weiss ,  Douglas S Williamson
Affiliations
  • 1. Vernalis (R&D) Ltd, 613 Reading Road, Winnersh, Wokingham RG41 5UA, UK.
PMID: 18407496 DOI: 10.1016/j.bmcl.2008.03.076
Abstract

We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.

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