In vivo morphological damage induced by a new benzimidazole prodrug in Echinococcus multilocularis metacestodes

J Pharm Sci. 1990 Jul;79(7):606-8. doi: 10.1002/jps.2600790713.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthelmintics / pharmacology*
  • Anthelmintics / therapeutic use
  • Benzimidazoles / pharmacology*
  • Benzimidazoles / therapeutic use
  • Echinococcosis / drug therapy
  • Echinococcosis / parasitology
  • Echinococcus / drug effects*
  • Echinococcus / ultrastructure
  • Gerbillinae
  • Male
  • Prodrugs
  • Thiourea / analogs & derivatives*
  • Thiourea / chemical synthesis
  • Thiourea / pharmacology

Substances

  • Anthelmintics
  • Benzimidazoles
  • Prodrugs
  • N-methoxycarbonyl N'-2-nitro-4-trifluoromethylphenyl thiourea
  • Thiourea