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6,7-二芳基蝶啶在三种实验模型中的杀线虫活性

Nematocide activity of 6,7-diarylpteridines in three experimental models.

作者信息

Ochoa C, Rodríguez M, Domínguez L, Saldaña J, Di Maio R, Alonso-Villalobos P, Martínez Grueiro M M

机构信息

Instituto de Química Médica (CSIC), Madrid, Spain.

出版信息

J Helminthol. 1999 Dec;73(4):333-6.

Abstract

The in vitro nematocide activity of seventeen 6,7-diarylpteridines has been tested using three different experimental models, Caenorhabditis elegans, Nippostrongylus brasiliensis and Heligmosomoides polygyrus. The method of evaluation of inhibition in the secretion of acetylcholinesterase by H. polygyrus seems to be the most indicated to avoid false positives. The in vivo activities, against Trichinella spiralis, of the most in vitro active pteridines have been assayed. All pteridine derivatives bearing 6,7-di-p-bromophenyl substituents have shown in vitro nematocide activities in the three experimental models used. Amongst all the pteridines tested in vivo, only 2,4-pteridinedithione derivatives exhibited moderate activity.

摘要

使用三种不同的实验模型——秀丽隐杆线虫、巴西日圆线虫和多枝细颈线虫,对17种6,7-二芳基蝶啶的体外杀线虫活性进行了测试。多枝细颈线虫乙酰胆碱酯酶分泌抑制的评估方法似乎最能避免假阳性。已测定了体外活性最高的蝶啶对旋毛虫的体内活性。所有带有6,7-二对溴苯基取代基的蝶啶衍生物在所用的三种实验模型中均表现出体外杀线虫活性。在所有体内测试的蝶啶中,只有2,4-蝶啶二硫酮衍生物表现出中等活性。

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