一种水溶性1,3,4-噻二唑类化合物的合成及生物活性

摘要

噻二唑与芳香醛反应制得一系列苯腙化合物,该类化合物再与氯乙酰氯反应得到关键中间体3,中间体3与三乙胺反应最终得到水溶性目标产物,对所有目标产物进行了红外、核磁氢谱、质谱和元素分析表征。水溶性实验证明,该类化合物在25℃的水中均具有大于10g的溶解度。并且生物活性实验表明,该类化合物对枯草杆菌(B． subtilis),大肠杆菌(E． coli),普通变形杆菌(P． vulgaris)和金黄色葡萄球菌(S． aureus)都具有明显的抑菌活性。%Different aldehydes was reacted with 1,3,4-thiadiazde to yield the phenylhydrazone. Then the phenylhydrazone were reac-ted with chloroacetyl chloride to yield the key intermediate 3. The title compounds were obtained by the reaction of 3 with triethyl-amine. All the title compounds were charactrized by elementary analysis,IR MS and 1 H NMR. Water-solubility experiment indicates that the title compounds displayed a good solubility above 10g in water at 25℃. At the same time,the results of biolofical activity tests showed that they all have activity on B. subtilis,E. coli,P. vulgaris and S. aureus.