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早有报道β-(5-硝基-2-呋喃)丙烯酸酯及酰胺类衍生物(Ⅰ)具有显著的抗日本血吸虫效力。为了寻觅疗效更高的药物和进一步研究结构与疗效的关系,鉴于多种吖啶类化合物均有抗菌杀虫活性,如引入吖啶环后有可能增强此类药物的抗日本血吸虫作用,为此,我们合成了一系列具有下列通式Ⅱ的吖啶丙烯酸酯及酰胺类衍生物。
It has been reported that β- (5-nitro-2-furan) acrylate and amido derivatives (I) have significant anti-Schistosoma japonicum efficacy. In order to find more effective drugs and to further study the relationship between structure and efficacy, in view of a variety of acridine compounds have antibacterial insecticidal activity, such as the introduction of acridine ring may enhance the anti-Schistosoma japonicum effect of such drugs, , We have synthesized a series of acridine acrylate and amide derivatives having the following general formula II.