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2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Moorjani M,Zhang X,Chen Y,Lin E,Rueter JK,Gross RS,Lanier MC,Tellew JE,Williams JP,Lechner SM,Malany S,Santos M,Ekhlassi P,Castro-Palomino JC,Crespo MI,Prat M,Gual S,Díaz JL,Saunders J,Slee DH

doi

10.1016/j.bmcl.2008.01.036

subject

Has Abstract

pub_date

2008-02-15 00:00:00

pages

1269-73

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00051-6

journal_volume

18

pub_type

杂志文章

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