期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 18, 页码 6590-6605出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.07.078
关键词
Adenosine receptor; Parkinson's disease; Pyrimidine carboxamide
Antagonists of the human A(2A) receptor have been reported to have potential therapeutic benefit in the alleviation of the symptoms associated with neurodegenerative movement disorders such as Parkinson's disease. As part of our efforts to discover potent and selective antagonists of this receptor, we herein describe the detailed optimization and structure-activity relationships of a series of pyrimidine-4-carboxamides. These optimized derivatives display desirable physiochemical and pharmacokinetic profiles, which have led to promising oral activity in clinically relevant models of Parkinson's disease. (C) 2009 Elsevier Ltd. All rights reserved.
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