取代酰肼类APN抑制剂的合成及初步活性测定  

The Synthesis and Preliminary Activity Assay in vitro of APN inhibitory

作　　者：朱慧婷[1] 刘婷[2] 李少华[3] 

机构地区：[1]江西省儿童医院药剂科,江西南昌330006 [2]宜春职业技术学院药学系,江西宜春336000 [3]南昌大学医学院药学系,江西南昌330006

出　　处：《江西化工》2011年第4期40-42,共3页Jiangxi Chemical Industry

摘　　要：以对位取代苯甲酸与氨基酸酯生成酰胺,然后肼解、闭环得到噁二唑酮,最后胺解得到目标化合物。合成的化合物经过IR、MS和H-NMR结构表征。这些化合物在体外对氨肽酶N显示了较好的抑制活性,可以作为先导化合物进行结构改造,为进一步研究APN抑制剂提供了新的方向。APN inhibitory derivatives were prepared from p - substituted benzoic acid and thiosemiearbazide in the presence of POCl3. The structures of the compounds were confirmed by IR, MS andtH -NMR. These compounds exhibited potent inhibitory activities against APN in vitro. These products can be modified as lead compounds and provide new methods for further research in enzyme inhibitors.

关 键 词：APN抑制剂 合成 抗癌活性 

分 类 号：TQ464.8[化学工程—制药化工]