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为了寻找口服抗丝虫病新药,合成了具有碳碳双键乙烯型和碳氮双键甲亚胺型两类化合物共95个。经感染棉鼠丝虫的棉鼠筛选结果,发现有25个化合物对微丝蚴和/或成虫具有明显的抗虫作用。其中以N-(5-硝基-2-呋喃甲叉)-1-氨基四氢-2(1H)嘧啶酮(Ⅱ_7)药理编号M-170对成虫有强烈的杀死作用,且毒性较低,已进入初步临床试验。
In order to find a new oral anti-filariasis medicine, a total of 95 compounds were synthesized with two types of compounds with carbon-carbon double bond ethylene type and carbon-nitrogen double bond azomethine type. Twenty-five compounds were found to have significant insect-resistant activity to microfilaria and / or adult worms following screening of cotton rats infected with the silkworm strain of cotton. Among them, M-170 was strongly killed by N- (5-nitro-2-furylidene) -1-aminotetrahydro-2 (1H) pyrimidinone (Ⅱ_7) , Has entered the preliminary clinical trial.