TY - JOUR
T1 - Anthelmintic activity of benzimidazole derivatives against Toxocara canis second-stage larvae and Hymenolepis nana adults
AU - Márquez-Navarro, Adrián
AU - Nogueda-Torres, Benjamín
AU - Hernández-Campos, Alicia
AU - Soria-Arteche, Olivia
AU - Castillo, Rafael
AU - Rodríguez-Morales, Sergio
AU - Yépez-Mulia, Lilián
AU - Hernández-Luis, Francisco
N1 - Funding Information:
This work was supported by grants from PAPIIT-UNAM IN210805 and CONACYT V43629-M.
PY - 2009/3
Y1 - 2009/3
N2 - 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%).
AB - 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%).
KW - Benzimidazole analogues
KW - Hymenolepis nana
KW - Prodrugs
KW - Toxocara canis
UR - http://www.scopus.com/inward/record.url?scp=59049097857&partnerID=8YFLogxK
U2 - 10.1016/j.actatropica.2008.11.014
DO - 10.1016/j.actatropica.2008.11.014
M3 - Artículo
C2 - 19073130
SN - 0001-706X
VL - 109
SP - 232
EP - 235
JO - Acta Tropica
JF - Acta Tropica
IS - 3
ER -