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

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

Affiliation

  • 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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