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ID: ALA1147529
Journal: Bioorg Med Chem Lett
Title: Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis.
Authors: Bauser M, Delapierre G, Hauswald M, Flessner T, D'Urso D, Hermann A, Beyreuther B, De Vry J, Spreyer P, Reissmüller E, Meier H.
Abstract: Adenosine kinase inhibition is an attractive therapeutic approach for several conditions for example, neurodegeneration, seizures, ischemia, inflammation and pain. Several nucleosidic and non-nucleosidic inhibitors are available. Using a virtual screening approach, we have discovered that 2-aryl oxazolo-pyrimidines are adenosine kinase inhibitors. Subsequent high throughput derivatization enabled the optimization of this new inhibitor chemotype resulting in highly potent derivatives. A variety of analogues were produced by applying liquid phase parallel synthesis to vary the 7-amino residues as well as the 2-aryl moiety.
CiteXplore: 15050645