Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays

  • Bioorg Med Chem Lett. 1999 Aug 16;9(16):2413-8. doi: 10.1016/s0960-894x(99)00398-4.
R M Campbell  1 ,  C Cartwright ,  W Chen ,  Y Chen ,  E Duzic ,  J M Fu ,  M Loveland ,  R Manning ,  B McKibben ,  C M Pleiman ,  L Silverman ,  J Trueheart ,  D R Webb ,  V Wilkinson ,  D J Witter ,  X Xie ,  A L Castelhano
Affiliations
  • 1. Cadus Pharmaceutical Corporation, Tarrytown, NY 10591, USA.
PMID: 10476879 DOI: 10.1016/s0960-894x(99)00398-4
Abstract

Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency.