Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9. doi: 10.1016/j.bmcl.2008.03.072.
Roger J Gillespie  1 ,  Ian A Cliffe ,  Claire E Dawson ,  Colin T Dourish ,  Suneel Gaur ,  Allan M Jordan ,  Antony R Knight ,  Joanne Lerpiniere ,  Anil Misra ,  Robert M Pratt ,  Jonathan Roffey ,  Gemma C Stratton ,  Rebecca Upton ,  Scott M Weiss ,  Douglas S Williamson
Affiliations
  • 1. Vernalis (R&D) Ltd, 613 Reading Road, Winnersh RG41 5UA, UK.
PMID: 18411049 DOI: 10.1016/j.bmcl.2008.03.072
Abstract

A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in an in vivo model of Parkinson's disease.

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