1,3,4-噻二唑衍生物的合成及初步活性测定  

The Synthesis and Preliminary Activity Assay in Vitro of 1,3,4-thiadiazole Derivarives

作　　者：李少华[1,2] 李刚[2] 黄惠明[2] 罗时远[2] 熊芳[3] 涂国刚[2] 刘成梅[1] 

机构地区：[1]南昌大学食品科学教育部重点实验室,江西南昌330031 [2]南昌大学医学院药学系,江西南昌330006 [3]南昌大学第二附属医院,江西南昌330006

出　　处：《南昌大学学报（理科版）》2009年第3期261-264,共4页Journal of Nanchang University(Natural Science)

基　　金：江西省自然基金资助项目(0620074);江西省教育厅课题(GJ09076);省卫生厅课题(20082015)

摘　　要：以对位取代苯甲酸与氨基硫脲为原料在三氯氧磷的条件下脱水,合成一系列5-芳基-2-氨基-1,3,4-噻二唑衍生物。合成的化合物经过IR、MS和1H-NMR结构表征。这些化合物在体外对氨肽酶N和基质金属蛋白酶显示了良好的抑制活性,可以作为先导化合物进行结构改造,为进一步研究蛋白酶抑制剂提供了新的方向。5 - Aryl - 1,3,4 - thiadiazol -2 - amine derivatives were prepared from p - substituted benzoic acid and thiosemicarbazide in the presence of POCl3. The structures of the compounds were confirmed by IR, MS and ^1H - NMR. These compounds exhibited potent inhibitory activities against APN and MMP in vitro. These products can be modified as lead compounds and provide new methods for further research in enzyme inhibitors.

关 键 词：1 3 4-噻二唑衍生物 合成 抗癌活性 

分 类 号：R914.2[医药卫生—药物化学]