Anthelmintic activity of benzimidazole derivatives against Toxocara canis second-stage larvae and Hymenolepis nana adults.
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%).
Márquez-Navarro
Adrián
A
Escuela Nacional de Ciencias Biológicas, IPN, México, D.F., Mexico.
Nogueda-Torres
Benjamín
B
Hernández-Campos
Alicia
A
Soria-Arteche
Olivia
O
Castillo
Rafael
R
Rodríguez-Morales
Sergio
S
Yépez-Mulia
Lilián
L
Hernández-Luis
Francisco
F
D015766:Albendazole / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D001562:Benzimidazoles / Q000032:analysis* / Q000494:pharmacology*; D005260:Female; D006925:Hymenolepiasis / Q000188:drug therapy; D048189:Hymenolepis nana / Q000187:drug effects*; D007814:Larva / Q000187:drug effects; D051379:Mice; D021261:Parasitic Sensitivity Tests; D017166:Toxocara canis / Q000187:drug effects*
D000871:Anthelmintics; D001562:Benzimidazoles; C031000:benzimidazole; D015766:Albendazole