噻吩骈[3,4-d]嘧啶-2,4-二酮类化合物对PDE的抑制作用

THE INHIBITION ACTIVITY OF THIENO [3,4-d] PYRIMIDINE-2,4-DIONE DERIVATIVES ON PHOSPHODIESTERASE

茶碱是一典型的磷酸二酯酶(PDE)抑制剂,结构类似核酸代谢物,易进入细胞内。口服、注射均易吸收,与腺苷酸(AMP),鸟苷酸(GMP)环化酶激动剂无交互作用,其副作用有恶心、胃肠道出血、中枢兴奋等。

On the basis of theophylline, a typical inhibitor on phosphodicsterasc (PDE), Thieno [3,4-d] pyrimidine-2, 4-dione derivatives, a novel kind of heterocyclic compounds, were designed and synthesized. Seven of eleven derivatives showed larger inhibiting activity to CaM-PDE than theophylline. As far as it goes, the inhibiting activty of YD_(13) with IC_(50) value 18 μmol/L is 190 times more than theophyllione (IC_(50)value 3100 μmol/L).