In vivo morphological damage induced by a new benzimidazole prodrug in Echinococcus multilocularis metacestodes.
Benzimidazoles are the most widely used compounds in chemotherapy of alveolar hydatid disease (AHD), but long-term administration is required to reach detectable plasma levels. N-Methoxycarbonyl N'-2-nitro 4-trifluoromethyl phenyl thiourea (2) was prepared as a potential prodrug of (5-trifluoromethyl-1H-benzimidazole-2-yl)-carbamic acid methyl ester. Biological effects of 2 were evaluated in gerbils (Meriones unguiculatus) against the causative agent of AHD, Echinococcus multilocularis metacestodes, through a transmission electron microscopy study. Significant morphological damage of tegument and protoscolices occurred after an 18-day treatment. The treatment of AHD by using the prodrug form of the benzimidazole deserves further study.
Walchshofer
N
N
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Lyon, France.
Delabre-Defayolle
I
I
Paris
J
J
Petavy
A F
AF
D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology* / Q000627:therapeutic use; D001562:Benzimidazoles / Q000494:pharmacology* / Q000627:therapeutic use; D004443:Echinococcosis / Q000188:drug therapy / Q000469:parasitology; D004446:Echinococcus / Q000187:drug effects* / Q000648:ultrastructure; D005849:Gerbillinae; D008297:Male; D011355:Prodrugs; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000871:Anthelmintics; D001562:Benzimidazoles; D011355:Prodrugs; C065703:N-methoxycarbonyl N'-2-nitro-4-trifluoromethylphenyl thiourea; D013890:Thiourea