Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.
Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.
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DOI：
10.1039/c6ob01149g
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发表时间：
2016-08-07
影响因子：
3.2
通讯作者：
Fernández PL
中科院分区：
文献类型：
--
作者：
Herrera L;Stephens DE;D'Avila A;George KG;Arman H;Zhang Y;Perry G;Lleonart R;Larionov OV;Fernández PL
在一系列新的双环和三环N-杂环的各种结构模式对主要利什曼原虫和巴拿马利什曼原虫的活性的影响进行了研究，并已确定在低微摩尔区域有活性的化合物。喹啉和四氢恶嗪吲哚（TOI）被证明有显着的抗利什曼原虫活性，而取代吲哚无活性。我们还表明，氯喹类似物诱导利什曼原虫杀死调节巨噬细胞活化。
Influence of various structural patterns in a series of novel bi- and tricyclic N-heterocycles on the activity against Leishmania major and Leishmania panamensis has been studied and compounds that are active in the low micromolar region have been identified. Both quinolines and tetrahydrooxazinoindoles (TOI) proved to have significant antileishmanial activities, while substituted indoles were inactive. We have also showed that a chloroquine analogue induces Leishmania killing by modulating macrophage activation.