Departamento de Química Inorgánica y Analitica, Laboratorio de radicales libres y antioxidantes, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago 1, Chile.
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5569-73. doi: 10.1016/j.bmcl.2012.07.013. Epub 2012 Jul 13.
In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. We have used the 4-hydroxycoumarin moiety (compound 1) as the molecular template for the synthesis of compounds 2-7. These derivates have shown moderate trypanocidal activity. However they have been proved to be good antioxidants. In particular compound 7 is the most active antioxidant and it is, therefore, a potential candidate for a successful employment in conditions characterized by free radicals overproduction.
在本通讯中，我们制备了一系列 6 种 4-羟基香豆素衍生物，槲皮素的结构类似物，槲皮素是一种抗氧化的天然化合物，目的是评估其对导致恰加斯病的寄生虫克氏锥虫的抗变形虫活性和抗氧化特性。我们使用 4-羟基香豆素部分（化合物 1）作为合成化合物 2-7 的分子模板。这些衍生物表现出中等的杀变形虫活性。然而，它们已被证明是良好的抗氧化剂。特别是化合物 7 是最有效的抗氧化剂，因此，它是一种有潜力的候选物，可以成功用于自由基过度产生的情况下。
