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

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.