title: Antischistosomal activity of N,N'-arylurea analogs against Schistosoma japonicum.
abstract: 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 22.6μM, and 7 of them had IC50 less than 10μM 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 200mg/kg or 400mg/kg to mice harboring S. japonicum.
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
authors: Houzong
authors: H
authors: Yao
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
authors: Fengyou
authors: F
authors: Liu
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
authors: Jinglei
authors: J
authors: Chen
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
authors: Yan
authors: Y
authors: Li
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
authors: Jinhao
authors: J
authors: Cui
authors: Jiangsu Key Laboratory of Preventive and Translational Medicine for Geriatric Diseases, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China. Electronic address: qiaochunhua@suda.edu.cn.
authors: Chunhua
authors: C
authors: Qiao
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D012549:Schistosoma japonicum / Q000187:drug effects*; D012556:Schistosomicides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D012556:Schistosomicides; D014508:Urea
keywords: Antischistosomal agents; Mice model; N,N′-Arylurea analogs; Schistosoma japonicum