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

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• 作者：Houzong Yao ; Fengyou Liu ; Jinglei Chen ; Yan Li ; Jinhao Cui ; Chunhua Qiao ; ^{qiaochunhua@suda.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Antischistosomal agents ; N ; N&prime ; -Arylurea analogs ; Schistosoma japonicum ; Mice model
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 March 2016
• 年：2016
• 卷：26
• 期：5
• 页码：1386-1390
• 全文大小：1571 K

文摘

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 μM, and 7 of them had IC₅₀ less than 10 μM 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.