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Discovery of potent and selective bicyclic A"2"B adenosine receptor antagonists via bioisosteric amide replacement

Paul Eastwood, Jacob Gonzalez, Sergio Paredes, Silvia Fonquerna, Arantxa Cardús, Juan Antonio Alonso, Arsenio Nueda, Teresa Domenech, Raquel F Reinoso, and Bernat Vidal

Bioorg Med Chem Lett 20(5):4 (2010) PMID 20138516

Several new potent and selective A"2"B adenosine receptor antagonists have been prepared in which the aryl-amide moiety of the lead series, exemplified by 1a, has been replaced by bioisosteric bicyclic moieties. Although the majority of compounds had generally improved microsomal stability as compared to 1a, this was not translated into overall improvements in the pharmacokinetic profiles of a representative set of compounds.

DOI: 10.1016/j.bmcl.2010.01.077
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