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二过氧螺环化合物对肝片形吸虫的活性。

The activity of dispiro peroxides against Fasciola hepatica.

机构信息

College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.

出版信息

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5320-3. doi: 10.1016/j.bmcl.2011.07.024. Epub 2011 Jul 19.

DOI:10.1016/j.bmcl.2011.07.024
PMID:21802291
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3159854/
Abstract

Dispiro 1,2,4-trioxanes and 1,2,4,5-tetraoxanes had superior efficacy against Fasciola hepatica than the corresponding ozonides (1,2,4-trioxolanes). For highest efficacy, spiroadamantane and carboxymethyl substructures were required. Three compounds completely cured F. hepatica-infected mice at single oral doses of 50mg/kg and two were partially curative at single doses of 25mg/kg.

摘要

二氧五环和四氧五环对肝片吸虫的疗效优于相应的臭氧化物（1,2,4-三氧杂环戊烷）。为了达到最高的疗效，需要螺环金刚烷和羧甲基取代基。三种化合物在 50mg/kg 的单次口服剂量下完全治愈了感染肝片吸虫的小鼠，两种化合物在 25mg/kg 的单次剂量下部分治愈。

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