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Anthelmintic activity of benzimidazole derivatives against Toxocara canis second-stage larvae and Hymenolepis nana adults |
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| Authors: | Adriá n Má rquez-Navarro,Alicia Herná ndez-Campos,Rafael Castillo,Liliá n Yé pez-Mulia |
| Affiliation: | a Escuela Nacional de Ciencias Biológicas, IPN, México 11340, D.F., Mexico b Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, México 04510, D.F., Mexico c Departamento de Sistemas Biológicos, División Ciencias Biológicas y de la Salud, UAM-X, México 04960, D.F., Mexico d Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, IMSS, México 06720, D.F., Mexico |
| Abstract: | 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 μM (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%). |
| Keywords: | Toxocara canis Hymenolepis nana Benzimidazole analogues Prodrugs |
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