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。
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 involved in the synthesis route. The compounds V a-1 showed varied inhibitory activity to PDE, and 3-methyl-1-o-methylbenzyl-5-amino-thieno [3,4-d] pyrimidine-2,4-dione was found to be more active.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1991年第3期142-144,共3页
Journal of China Pharmaceutical University
关键词
嘧啶粉衍生物
合成
抑酶活性
Thieno [3,4-d] pyrimidine-2,4-dione
Phosphodiesterase inhibitor
Theophylline
