Bioorg Med Chem Lett 1999 Aug 16;9(16):2413-8
Selective A1-adenosine receptor antagonists identified using yeast
Saccharomyces cerevisiae functional assays.
Campbell RM, Cartwright C, Chen W, Chen Y, Duzic E, Fu JM, Loveland M, Manning R, McKibben B, Pleiman
CM, Silverman L, Trueheart J, Webb DR, Wilkinson V, Witter DJ, Xie X, Castelhano AL
Cadus Pharmaceutical Corporation, Tarrytown, NY 10591, USA.
[Medline record in process]
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. |
