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Bioorg Med Chem Lett. 2008 Feb 15;18(4):1269-73. doi: 10.1016/j.bmcl.2008.01.036. Epub 2008 Jan 13.

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

Author information

1
Department of Medicinal Chemistry, Neurocrine Biosciences, 12790 El Camino Real, San Diego, CA 92130, USA.

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.

PMID:
18249540
DOI:
10.1016/j.bmcl.2008.01.036
[Indexed for MEDLINE]

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