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

作者信息

Walchshofer N, Delabre-Defayolle I, Paris J, Petavy A F

机构信息

Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Lyon, France.

出版信息

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

DOI:10.1002/jps.2600790713
PMID:2118956
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.

摘要

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