期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 3, 页码 967-971出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.075
关键词
Adenosine A(2a); Parkinson's disease; 1,2,4-Triazolo[1,5-c]pyrimidine
Antagonism of the adenosine A(2a) receptor offers great promise in the treatment of Parkinson's disease. In the course of exploring pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, which led to clinical candidate SCH 420814, we prepared 1,2,4-triazolo[1,5-c]pyrimidines with potent and selective (vs A(1)) A(2a) antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure-activity relationships and plasma levels are described for this series. (C) 2008 Elsevier Ltd. All rights reserved.
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