synthesis 1-acyl-3-(2-aminophenyl) thioureas as anti-intestinal nematode prodrugs合成1-acyl-3 -(2 -aminophenyl)硫脲anti-intestinal线虫高活性化合物.pdf

Molecules 2010, 15, 6941-6947; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis 1-Acyl-3-(2-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs Li-Ping Duan, Jia Xue, Li-Li Xu and Hao-Bing Zhang * National Institute for Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai, 200025, China * Author to whom correspondence should be addressed; E-Mail: zhanghaobing@. Received: 4 August 2010; in revised form: 6 September 2010/ Accepted: 25 September 2010 / Published: 8 October 2010 Abstract: A series of 1-acyl-3-(2-aminophenyl) thiourea derivatives were designed and synthesized. The structures of all the newly synthesized compounds were identified by IR, elemental analysis, 1H-NMR and 13C-NMR. Their anti-intestinal nematode activities against Nippostrongylus brazilliensis were evaluated in rats by an oral route. Among these compounds, at concentrations of 10 mg/kg of rat, compound (1-(2-furanyl)acyl-3- (2- aminophenyl) thiourea) (5h) produced the highest activity with 89.4% deparasitization. The present work suggests that 1-acyl-3-(2-aminophenyl) thiourea derivatives may become useful lead compounds for anti-intestinal nematode treatment. Keywords: acyl; thiourea; deparasitization; Nippostrongylus brazilliensis 1. Introduction Mebendazole and albendazole have been used against human and animal helminth parasites fo