磷酸二酯酶抑制剂吡唑并[4,3-d]嘧啶-7-酮类衍生物的研究

Studies of phosphodiesterase inhibitors pyrazolo[4,3-d] pyrimidin-7-one derivatives

目的寻找新型磷酸二酯酶抑制剂 ,设计合成未见文献报道的吡唑并 [4 ,3 d]嘧啶 7 酮类衍生物。方法合成了 8个新的衍生物 ,结构经IR、1H NMR和MS确证 ,并进行离体主动脉条和离体气管螺旋条药理实验。结果目标化合物均具有一定的血管扩张作用和支气管扩张作用 ,其中 ,Ⅸc的血管扩张作用优于对照药维拉帕米 ,Ⅸa的支气管扩张作用强于对照药氨茶碱。结论吡唑并[4 ,3 d]嘧啶 7

Aim New pyrazolopyrimidin 7 one derivatives were to be designed and synthesized in order to find a new type of phosphodiesterase inhibitors.Method A series of new pyrazolopyrimidin 7 one derivatives was synthesized and their chemical structures were comfirmed by IR, 1H NMR and MS.They were tested for their pharmacological activity by the isolated rabbit thoracic aorta experiment and the isolated guinea pig tracheal chain experiments.Results All of the topic compounds had some angiectatic activity and bronchiectatic activity.The angiectatic activity of Ⅸc and the bronchiectatic activity of Ⅸa were more potent than that of their each control compound verapamil and aminophylline.Conclusion Pyrazolopyrimidin 7 one derivatives were probably developed to be a new type of selective phosphodiesterase inhibitors