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噻吩衍生物具有多种多样生物活性,有的作为消毒杀菌剂,也有作为驱蠕抗虫药物。3,4,5-三氯噻吩-2-磺酰氯有抗菌杀虫作用,2-(5-硝基-2-噻吩)-4-取代噻唑、噻嘧啶以及214-二氨基-噻吩-3-甲酸均属于驱蠕虫药物。我国最近发现的N-(5-硝基-2-呋喃甲叉)-1-氨基四氢-2(1H)嘧啶酮(简称呋喃嘧酮)对丝虫微丝蚴和成虫均有较强的杀灭作用。经试用于临床证明有较好疗效。为了提高杀虫效力,减低副反应,以其同电异素体噻吩代替呋喃合成了具有下述通式(Ⅰ)的化合物(图1),进行药理试验。
Thiophene derivatives have a variety of biological activity, and some as a disinfectant, but also as deworming insect-resistant drugs. 3,4,5-trichloro-thiophene-2-sulfonyl chloride antibacterial insecticidal effect of 2- (5-nitro-2-thiophene) -4-substituted thiazoles, pyrantel and 214-diamino- Formic acid belongs to the drive worms drugs. China recently discovered N- (5-nitro-2-furylidene) -1- aminotetrahydro-2 (1H) pyrimidinone (furanone) on filarial microfilariae and adults have a strong Kill the effect. The trial proved to have good clinical effect. In order to improve insecticidal efficacy and reduce side effects, a compound having the following general formula (I) was synthesized using its electropartile thiophene instead of furan (Figure 1) and subjected to pharmacological tests.