新型四唑[1,5-a]并嘧啶-5,7-二醇衍生物的合成及对Cdc25B抑制活性评价  

Synthesis and Cdc25B Inhibitory Activity Evaluation of Novel Tetrazolo[1,5-a]Pyrimidin-5,7-diol Derivatives

作　　者：杨娜[1] 鲁源 张晓晖[1] YANG Na;LU Yuan;ZHANG Xiaohui(Department of Pharmacy, The Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, China;College of Pharmacology, Inner Mongolia Medical University, Hohhot 010059, China)

机构地区：[1]内蒙古医科大学附属医院药剂部,内蒙古呼和浩特010050 [2]内蒙古医科大学药学院,内蒙古呼和浩特010059

出　　处：《合成化学》2022年第7期556-562,共7页Chinese Journal of Synthetic Chemistry

基　　金：内蒙古自治区自然科学基金资助项目(2017MS0898)。

摘　　要：以5-氨基四唑与丙二酸二乙酯为原料设计并合成了四唑[1,5-a]并嘧啶-5,7-二醇(1)和13个新型6-芳基偶氮四唑[1,5-a]并嘧啶-5,7-二醇(2a~2m)。通过^(1)H NMR,^(13)C NMR,IR,ESI-MS和元素分析等方法对其进行了结构表征。对所合成的目标化合物进行了细胞分裂周期25B磷酸酶(Cdc25B)抑制活性筛选,结果表明:化合物2b,2c,2h,2i和2m对Cdc25B具有抑制作用,其抑制率可高达97.66%。Tetrazolo[1,5-a]pyrimidin-5,7-diol(1)and thirteen novel tetrazolo[1,5-a]pyrimidin-5,7-diol derivatives(2a~2m)were synthesized in the basis of 5-aminotetrazole and diethyl malonate.The structures of the compounds were characterized by ^(1)H NMR,^(13)C NMR,IR,ESI-MS and elemental analysis.All synthesized target compounds were screened for their inhibitory activity against cell division cycle 25B phosphatase(Cdc25B).The results show that compounds 2b,2c,2h,2i and 2m exhibited good activities against Cdc25B,the inhibition rates up to 97.66%.

关 键 词：5-氨基四唑 丙二酸二乙酯 四唑[1 5-a]并嘧啶 有机合成 Cdc25B抑制剂 

分 类 号：O626[理学—有机化学]