2. Academic Validation
  3. Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays

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

Affiliation

  • 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.

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