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Bioorg Med Chem Lett
; 18(4): 1269-73, 2008 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18249540
RESUMO
In this report, the design and synthesis of a series of pyrimidine based adenosine A(2A) antagonists are described. The strategy and outcome of expanding SAR exploration to attenuate hERG and improve selectivity over A(1) are discussed. Compound 33 exhibited excellent potency, selectivity over A(1), and reduced hERG liability.