发现 N-(5,6-二芳基吡啶-2-基)酰胺衍生物作为强效和选择性 A(2B)腺苷受体拮抗剂。
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
机构信息
Almirall Research Center, Almirall S.A., Ctra. Laureà Miró 408, St. Feliu de Llobregat, E-08980 Barcelona, Spain.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700. doi: 10.1016/j.bmcl.2010.01.045. Epub 2010 Jan 20.
PMID:20137946
Abstract
The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A(2B) adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.
摘要
描述了一系列 N-(5,6-二芳基吡啶-2-基)酰胺衍生物作为有效 A(2B)腺苷受体拮抗剂的合成和 SAR 研究。几种化合物对其他腺苷受体具有良好的选择性。具有强效和选择性的类似物 9 在大鼠中表现出良好的口服生物利用度。
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