Divergent solution-phase synthesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists.
A practical and divergent solution-phase synthetic strategy has been optimized to prepare a highly diverse library of 2,4-diaryl- and 2,6-diarylpyrimidines. Structural elaboration of the starting heterocyclic scaffolds was accomplished by exploiting the potential for diversity offered by the Suzuki-Miyaura cross-coupling reaction. These studies enabled the identification of structurally simple, highly potent, and selective A(3) adenosine receptor antagonists.
Yaziji
Vicente
V
Combinatorial Chemistry Unit and Screening Unit, Institute of Industrial Pharmacy, University of Santiago de Compostela, Santiago de Compostela, Spain.
Coelho
Alberto
A
El Maatougui
Abdelaziz
A
Brea
José
J
Loza
M Isabel
MI
Garcia-Mera
Xerardo
X
Sotelo
Eddy
E
D058918:Adenosine A3 Receptor Antagonists; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D006801:Humans; D011485:Protein Binding; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D043684:Receptor, Adenosine A3 / Q000378:metabolism
D058918:Adenosine A3 Receptor Antagonists; D011743:Pyrimidines; D043684:Receptor, Adenosine A3