亚甲基胺取代的芳基并嘧啶作为有效的腺苷 A(2A)/A(1)拮抗剂。
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
机构信息
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., Welsh and McKean Roads, PO Box 776, Spring House, PA 19477, United States.
出版信息
Bioorg Med Chem Lett. 2010 May 1;20(9):2864-7. doi: 10.1016/j.bmcl.2010.03.042. Epub 2010 Mar 11.
PMID:20347304
Abstract
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally.
摘要
研究人员鉴定出一系列新型芳基茚并嘧啶类化合物为 A(2A)和 A(1)受体拮抗剂。该系列化合物通过在 8 位和 9 位引入亚甲基胺取代基，使体外活性得到优化。当以口服方式给予这些化合物时，它们在帕金森病的小鼠模型中表现出优异的活性。
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