The activity of dispiro peroxides against Fasciola hepatica.

The activity of dispiro peroxides against Fasciola hepatica.
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二螺过氧化物对肝片形吸虫的活性。

DOI:
10.1016/j.bmcl.2011.07.024
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发表时间:
2011
影响因子:
2.7
通讯作者:
Vennerstrom,JonathanL
Vennerstrom,JonathanL
中科院分区:
医学4区
文献类型:
--
作者:
Wang,Xiaofang;Zhao,Qingjie;Vargas,Mireille;Dong,Yuxiang;Sriraghavan,Kamaraj;Keiser,Jennifer;Vennerstrom,JonathanL

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双螺环1,2,4-三恶烷和1,2,4,5-四恶烷对肝片吸虫的疗效上级相应的臭氧化物(1,2,4-三恶烷)。为了获得最高功效,需要螺金刚烷和羧甲基亚结构。三种化合物完全治愈F.单次口服剂量为50 mg/kg时,有2只感染了肝炎的小鼠,单次口服剂量为25 mg/kg时,有2只部分治愈。
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.