13142-48-8Relevant academic research and scientific papers
Antischistosomal activity of N,N′-arylurea analogs against Schistosoma japonicum
Yao, Houzong,Liu, Fengyou,Chen, Jinglei,Li, Yan,Cui, Jinhao,Qiao, Chunhua
supporting information, p. 1386 - 1390 (2016/02/19)
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.
Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists
Bromidge, Steven M.,Dabbs, Steven,Davies, David T.,Davies, Susannah,Duckworth, D.Malcolm,Forbes, Ian T.,Gadre, Angela,Ham, Peter,Jones, Graham E.,King, Frank D.,Saunders, Damian V.,Thewlis, Kevin M.,Vyas, Deepa,Blackburn, Thomas P.,Holland, Vicky,Kennett, Guy A.,Riley, Graham J.,Wood, Martyn D.
, p. 2767 - 2773 (2007/10/03)
A model series of 5-HT(2C) antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N'-pyridin-3-yl ureas were found to have a range of 5-HT(2C) receptor affinities and selectivities over the closely related 5-HT(2A) receptor. Extrapolation of simple SAR, derived from this set of compounds, to the more active but synthetically more complex 1-(3-pyridyl-carbamoyl)indoline series allowed us to target optimal substitution patterns and identify potent and selective 5-HT(2C/2B) antagonists. Copyright (C) 1999 Elsevier Science Ltd.
