期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 4, 页码 1269-1273出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.036
关键词
A(2A) antagonists; adenosine receptor; Parkinson's disease; phenacylaminopyrimidines; hERG
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 A1, and reduced hERG liability. (c) 2008 Elsevier Ltd. All rights reserved.
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