双环和三环 N-杂环类化合物抗利什曼原虫活性的结构模式分析。
Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles.
机构信息
Centro de Biología Molecular y Celular de Enfermedades, Instituto de Investigaciones Científicas y de Alta Tecnología (INDICASAT-AIP), Edificio 219, Ciudad del Saber, Apartado 0843-01103, Panamá, República de Panamá.
出版信息
Org Biomol Chem. 2016 Aug 7;14(29):7053-60. doi: 10.1039/c6ob01149g. Epub 2016 Jul 4.
Abstract
The 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.
摘要
研究了一系列新型双环和三环 N-杂环中各种结构模式对大疱性表皮松解症和巴拿马利什曼原虫活性的影响，并确定了在低微摩尔区域具有活性的化合物。喹啉和四氢恶唑并吲哚（TOI）都被证明具有显著的抗利什曼原虫活性，而取代的吲哚则没有活性。我们还表明，氯喹类似物通过调节巨噬细胞的激活诱导利什曼原虫的杀伤。
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