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

نویسندگان

  • Roger J Gillespie
  • 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
چکیده

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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Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 18 9  شماره 

صفحات  -

تاریخ انتشار 2008