论文部分内容阅读
呋喃烯唑(S-72055)经动物实验和临床观察,证明对日本血吸虫病有较好的疗效,为了寻找更好的药物,本文以β-(5-硝基-2-呋喃)丙烯酰胺肟为原料,合成了若干系列呋喃烯唑的类似物。同时,为了研究乙烯桥在呋喃烯唑结构中的重要性,又以5-硝基-2-呋喃甲酰胺肟为原料,合成了呋喃烯唑的去乙烯桥的类似物。动物实验结果,证明(口恶)二唑环上5位酰胺基或5位烃氨甲基的存在,一般可使化合物具有抗血吸虫作用,而呋喃烯唑的去乙烯桥类似物,几乎没有活性。
Furazole (S-72055) has been proved to be effective in treating schistosomiasis japonica by animal experiments and clinical observations. In order to find a better drug, this paper takes beta- (5-nitro-2-furan) As a starting material, several series of analogues of furantrole were synthesized. At the same time, in order to study the importance of vinyl bridge in the structure of furazole, the 5-nitro-2-furancarboxamide oxime was used as the starting material to synthesize the analogues of furanoleazole to ethylene. The animal experiments show that the presence of the 5-position amido group or the 5-position hydrocarbon aminomethyl group on the oxadiazole ring generally results in the compounds having an anti-schistosome effect whereas the deethin bridge analogs of the furanolezole have little activity .