☆ 4.5 Article

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

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

类别

Chemistry, Medicinal Chemistry, Organic

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摘要

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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