期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 9, 页码 2916-2919出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.075
关键词
adenosine A(2A) receptor; Parkinson's disease; mefloquine
The (-)-(11R,2'S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A(2A) receptor antagonist. Further investigation of this compound has led to the discovery of a series of keto-aryl thieno[3,2-d]pyrimidine derivatives, which are potent and selective antagonists of the adenosine A(2A) receptor. These derivatives show selectivity against the A(1) receptor. Furthermore, some of these compounds have been shown to have in vivo activity in a commonly used model, suggesting the potential for the treatment of Parkinson's disease. (C) 2008 Elsevier Ltd. All rights reserved.
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