Synthesis 1-Acyl-3-(2'-aminophenyl) thioureas as Anti-Intestinal Nematode Prodrugs

Molecules

Li-Ping Duan¹  Jia Xue¹  Li-Li Xu¹ 

[1] National Institute for Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai, 200025, China

关键词: acyl;    thiourea;    deparasitization;    Nippostrongylus brazilliensis;   

DOI  :  10.3390/molecules15106941

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.