吡啶并[2,3 - d]嘧啶 - 2,4 - 二酮作为磷酸二酯酶4（PDE 4）抑制剂的合成与评价
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
作者信息
Nam G, Yoon C M, Kim E, Rhee C K, Kim J H, Shin J H, Kim S H
机构信息
Biochemicals Research Center, Korea Institute of Science and Technology, Cheongryang, Seoul, South Korea.
出版信息
Bioorg Med Chem Lett. 2001 Mar 12;11(5):611-4. doi: 10.1016/s0960-894x(00)00681-8.
Abstract
The syntheses and in vitro evaluation of a new series of pyrido[2,3-d]pyrimidine-2,4-diones bearing substituents at C-3 and/or C-4 positions on the pyridine ring are described. Some of these compounds, especially 51 and 6f, were found to be potent phosphodiesterase 4 (PDE 4) inhibitors exhibiting improved ratio of PDE 4 inhibitory activity:rolipram binding assay (RBA).
摘要
描述了一系列在吡啶环的C-3和/或C-4位带有取代基的新型吡啶并[2,3-d]嘧啶-2,4-二酮的合成及体外评价。发现其中一些化合物，尤其是51和6f，是有效的磷酸二酯酶4（PDE 4）抑制剂，在PDE 4抑制活性与咯利普兰结合试验（RBA）中表现出改善的比率。
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