title: Divergent solution-phase synthesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists.
abstract: 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.
authors.affiliation: Combinatorial Chemistry Unit and Screening Unit, Institute of Industrial Pharmacy, University of Santiago de Compostela, Santiago de Compostela, Spain.
authors.forename: Vicente
authors.initials: V
authors.lastname: Yaziji
authors.forename: Alberto
authors.initials: A
authors.lastname: Coelho
authors.forename: Abdelaziz
authors.initials: A
authors.lastname: El Maatougui
authors.forename: José
authors.initials: J
authors.lastname: Brea
authors.forename: M Isabel
authors.initials: MI
authors.lastname: Loza
authors.forename: Xerardo
authors.initials: X
authors.lastname: Garcia-Mera
authors.forename: Eddy
authors.initials: E
authors.lastname: Sotelo
mesh_terms: 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
chemical_list: D058918:Adenosine A3 Receptor Antagonists; D011743:Pyrimidines; D043684:Receptor, Adenosine A3