Márquez-Navarro Adrián, Nogueda-Torres Benjamín, Hernández-Campos Alicia, Soria-Arteche Olivia, Castillo Rafael, Rodríguez-Morales Sergio, Yépez-Mulia Lilián, Hernández-Luis Francisco
Escuela Nacional de Ciencias Biológicas, IPN, México, D.F., Mexico.
Acta Trop. 2009 Mar;109(3):232-5. doi: 10.1016/j.actatropica.2008.11.014. Epub 2008 Nov 25.
The anthelmintic activity of 11 benzimidazole derivatives (A1-A11) and 2 thioureides N,N'-disubstituted (B1-B2) was determined. Each compound and albendazole was tested in vitro against Toxocara canis larvae and in vivo against Hymenolepis nana adult. Compounds A1-A6 and B1-B2 were designed as albendazole prodrugs. Compounds A8-A11 were designed as direct analogues of A7, which had previously proved to be an effective agent against Fasciola hepatica. Results of the in vitro screening showed that A6 was more active than albendazole at 0.18 microM (relative mobility 40% and 80%, respectively). Whereas that the in vivo evaluation against H. nana, compounds A7-A11 demonstrated significant activity in terms of removing cestode adults in the range of 88-97%, displaying better efficacy than albendazole (83%).
测定了11种苯并咪唑衍生物(A1 - A11)和2种N,N'-二取代硫脲(B1 - B2)的驱虫活性。每种化合物和阿苯达唑都在体外针对犬弓首蛔虫幼虫进行了测试,并在体内针对微小膜壳绦虫成虫进行了测试。化合物A1 - A6和B1 - B2被设计为阿苯达唑前药。化合物A8 - A11被设计为A7的直接类似物,A7先前已被证明是一种有效的抗肝片吸虫剂。体外筛选结果表明,在0.18微摩尔浓度下,A6比阿苯达唑更具活性(相对迁移率分别为40%和80%)。而在针对微小膜壳绦虫的体内评估中,化合物A7 - A11在清除绦虫成虫方面表现出显著活性,清除率在88 - 97%之间,显示出比阿苯达唑(83%)更好的疗效。