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.
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. |
