【摘要】 目的合成含有酰胺基团的硝基呋喃衍生物,并进行小白鼠体外筛选和体内抗日本血吸虫活性测试。方法以四氢呋喃为溶剂,N,N’-二环己基碳二亚胺为缩合剂,5-硝基呋喃甲酸与1-羟基-苯并三氮唑(HOBt)缩合得到中间体,该中间体与胺缩合得到硝基呋喃酰胺类目标化合物。结果与结论合成了11个硝基呋喃酰胺类化合物,其中6个是未见文献报道的新化合物。抗日本血吸虫活性评价结果显示,有7个化合物对血吸虫具有一定的抑制效果,尤其是化合物N’-(2-吗啡啉基乙基)-5-硝基呋喃-2-酰肼(6k),抗虫效果最显著,可作为抗血吸虫的先导化合物做进一步研究。更多还原

【Abstract】 In view of rapid re-infection following treatment and concern about the development of tolerance and/or resistance to praziquante, there is an urgent need for research and development of novel drugs for the prevention and treatment of Schistosomiasis. Eleven novel 5-nitrofuran amides were designed and synthesized by condensation reation from 5-nitrofuran formic acid,amines using DCC as dehydrating agent and HOBt as catalytic agent in THF. The structures of target products were confirmed by ESI-MS,NMR and elemental analysis. Seven target compounds had a positive influence on anti-schistosomiasis activity. The result showed that compound 6 k had the best effect on anti-schistosomiasis activity. The compound 6 k can be used as the lead compound against Schistosoma japonicum for futher research.更多还原