Antischistosomal activity of N,N '-arylurea analogs against Schistosoma japonicum

作者：Yao, Houzong; Liu, Fengyou; Chen, Jinglei; Li, Yan; Cui, Jinhao; Qiao, Chunhua^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(5): 1386-1390.

DOI：10.1016/j.bmcl.2016.01.075

• Antischistosomal agents
• N,N'-Arylurea analogs
• Schistosoma japonicum
• Mice model

Although the antischistosomal activities of N,N'-arylurea analogs were reported, systematic structure-activity relationships have not been conducted. In this Letter, we reported the design, synthesis and evaluation of 45 N,N'-arylurea analogs. Among these prepared compounds, 13 compounds were urea linker modified and 32 were N,N'-arylurea derivatives. The activity evaluation revealed 12 analogs exhibited IC50 values lower than 22.6 mu M, and 7 of them had IC50 less than 10 mu M against the juvenile Schistosoma japonicum in vitro. Their worm killing potency was even higher against adult worm. Unfortunately, low to moderate worm burden reduction of 0-33.4% was recorded after administration of a single oral dose of 200 mg/kg or 400 mg/kg to mice harboring S. japonicum.

• 出版日期2016-3-1
• 单位苏州大学