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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。
OBJECTIVE To synthesize nitrofuran derivatives containing amide groups and in vitro screening and in vivo anti-Schistosoma japonicum activity test in mice. Methods Condensation of 5-nitrofuric acid and 1-hydroxy-benzotriazole (HOBt) with tetrahydrofuran as solvent and N, N’-dicyclohexylcarbodiimide as condensing agent gave the intermediate Condensation of the amine gives the nitro-furan amide target compound. RESULTS AND CONCLUSIONS Eleven nitro-furanides were synthesized, of which six were new compounds not reported in the literature. The results of anti-schistosoma japonicum activity evaluation showed that seven compounds had some inhibitory effect on schistosome, especially the compound N ’- (2-morpholinoethyl) -5-nitrofuran-2-hydrazide The most significant anti-insect effect can be used as a precursor compound of anti-schistosome for further study.