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

Although the antischistosomal activities of N,N’-arylurea analogs were reported, systematic structure-activity relationships have not been conducted. In this paper, 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 Schistosom japonicum in vitro. Their worm killing potency was even higher against adult worm. Unfortunately, low to moderate worm burden reduction of 0 to 33.4% was recorded after administration of a single oral dose of 200 mg/kg or 400 mg/kg to mice harboring S. japonicum.