噻吩骈嘧啶二酮衍生物的合成及其抑酶活性

Synthesis and Inhibitor Activity to Phosphodiesterase of Thieno 3, 4-d Pyrimidine-2,4-Dione Derivatives

摘要: 为了寻找新的磷酸二酯酶(PDE)抑制剂,以茶碱为先导化合物,氰乙酸和氨基甲酸乙酯为原料,经中间体N-取代-5-氰基脲嘧啶,合成了12个噻吩骈3,4-d嘧啶-2,4-二酮类化合物。它们对PDE有不同程度的抑制活性,其中3-甲基-1-邻甲基苯基-5-氨基噻吩骈3,4-d嘧啶-2,4-二酮活性较强。

Abstract: In search of novel phosphodiesterase (PDE) inhibitors, twelve compounds of thieno 3,4-d pyrimidiine-2,4-diones (V a-1) were designed and synthesized with cyanoacetic aicd and urethan taken as the starting materials. Condensation and cyclization were inv