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合成及三氟拉林类似物的生物评价作为抗利什曼原虫药物。

Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents.

机构信息

Department of Chemical Industry Technologies, INETI, Estrada do Paço do Lumiar, 1649-038 Lisboa, Portugal.

出版信息

Bioorg Med Chem. 2010 Jan 1;18(1):274-81. doi: 10.1016/j.bmc.2009.10.059. Epub 2009 Oct 31.

Abstract

A series of new analogues of trifluralin (TFL) were synthesized and characterized in view of changing the unfavorable properties that limits its use as antileishmanial agent. Some of the TFL analogues display more activity than a standard drug (miltefosine) against the promastigote forms of Leishmania infantum and Leishmania donovani and the intracellular form (THP-1 infected with L. infantum). All analogues showed a clear advantage over miltefosine, as they are not hemolytic. Some analogues can conjugate these characteristics with reduced cell toxicity and improved intracellular activity.

摘要

为了改变三氟拉林(TFL)作为抗利什曼原虫药物的不利性质,我们合成并表征了一系列新的 TFL 类似物。一些 TFL 类似物对利什曼原虫和杜氏利什曼原虫的前鞭毛体形式和细胞内形式(感染利什曼原虫的 THP-1)的活性比标准药物(米替福新)更高。所有类似物都显示出比米替福新更明显的优势,因为它们没有溶血作用。一些类似物可以将这些特性与降低细胞毒性和提高细胞内活性结合起来。

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