期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 3, 页码 1090-1093出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.028
关键词
Adenosine; A(2A); A(2A) receptor; A(2A) antagonist; A(2A) receptor antagonist; Parkinson's disease
A series of benzofuran derivatives were prepared to study their antagonistic activities to the A(2A) receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modi. cations of the amide moiety showed enhanced antagonistic activity. From these studies, compounds 13c, 13f, and 24a showed good potency in vitro and were identified as novel A(2A) receptor antagonists suitable for oral activity evaluation in animal models of catalepsy. (C) 2009 Elsevier Ltd. All rights reserved.
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