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  • Tuesday, June 21, 2005
  • New Pyrrolo[2,1-f]purine-2,4-dione and Imidazo[2,1-f]purine-2,4-dione Derivatives as Potent and Selective Human A3 Adenosine Receptor Antagonists
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  • Compounds presenting an additional fused ring on the xanthine nucleus have been reported to exhibit antagonistic activity with various levels of affinity and selectivity toward the four adenosine receptors subtypes A1, A2A, A2B, and A3. This paper reports synthesis and biological evaluation of new 1-benzyl-3-propyl-1H,6H-pyrrolo[2,1-f]purine-2,4-diones and 1-benzyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-diones, among which we identified potent and selective A3 adenosine receptors antagonists. In particular, 1-benzyl-7-methyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-dione (11e) shows a Ki (hA3) value from binding assay of 0.8 nM.


    J. Med. Chem., 2005, 48 (14), pp 4697–4701
    DOI: 10.1021/jm058008c
    Publication Date (Web): June 21, 2005
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Abdel-Naser Mohammad Tawfeeq Zaid
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