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Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays. |
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| Authors: | R M Campbell 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 |
| Affiliation: | Cadus Pharmaceutical Corporation, Tarrytown, NY 10591, USA. |
| 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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