期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 5, 页码 1399-1402出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.042
关键词
Adenosine; GPCR; Purinone; SAR; Parkinson's disease
A series of trisubstituted purinones was synthesized and evaluated as A(2A) receptor antagonists. The A2A structure-activity relationships at the three substituted positions were studied and selectivity against the A(1) receptor was investigated. One antagonist 12o exhibits a K-i of 9 nM in an A(2A) binding assay, a K-b of 18 nM in an A2A cAMP functional assay, and is 220-fold selective over the A1 receptor. (C) 2009 Elsevier Ltd. All rights reserved.
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