|
|||||
|
|
| 1,3,4-噻二唑衍生物的合成及初步活性测定 | |
| 引用本文： | 李少华,李刚,黄惠明,罗时远,熊芳,涂国刚,刘成梅.1,3,4-噻二唑衍生物的合成及初步活性测定[J].南昌大学学报(理科版),2009,33(3). |
| 作者姓名： | 李少华 李刚 黄惠明 罗时远 熊芳 涂国刚 刘成梅 |
| 作者单位： | 1. 南昌大学,食品科学教育部重点实验室,江西,南昌,330031;南昌大学,医学院药学系 2. 南昌大学,医学院药学系 3. 南昌大学,第二附属医院,江西,南昌,330006 4. 南昌大学,食品科学教育部重点实验室,江西,南昌,330031 |
| 基金项目： | 江西省自然科学基金，江西省教育厅课题，省卫生厅课题 |
| 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. |
| 关 键 词： | 1 3 4-噻二唑衍生物 合成 抗癌活性 |
The Synthesis and Preliminary Activity Assay in Vitro of 1,3,4-thiadiazole Derivarives |
|
| LI Shao-hua,LI Gang,HUANG Hui-ming,LUO Shi-yuan,XIONG Fang,TU Guo-gang,LIU Cheng-mei.The Synthesis and Preliminary Activity Assay in Vitro of 1,3,4-thiadiazole Derivarives[J].Journal of Nanchang University(Natural Science),2009,33(3). | |
| Authors: | LI Shao-hua LI Gang HUANG Hui-ming LUO Shi-yuan XIONG Fang TU Guo-gang LIU Cheng-mei |
| Institution: | a.State Key Laboratory of Food Science and Technology;Nanchang University;Nanchang 330031;China;b.Department of Pharmacy;NanChang University Medical College;NanChang 330006;c.Department of Cardiology;the Second Affiliated Hospital of NanChang University;China |
| Abstract: | 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. |
| Keywords: | 1 3 4-thiadiazole derivative synthesis antitumor activity |
| 本文献已被 CNKI 万方数据 等数据库收录！ | |