Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001, Heverlee, Belgium.
Molecules. 2012 Oct 18;17(10):12243-51. doi: 10.3390/molecules171012243.
We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values of 6.25-12.5 µM. Compounds 1 and 5 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata (MFC < 50 µM). The 6-amide derivatives 1, 2, 5, and 6 and the 6-urea derivatives 10, 12, 13 and 15 could also eradicate C. albicans biofilms. We found that the 6-urea derivatives 10, 13, and 15 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms.
我们已经确定了 2,6-二取代喹啉的两个亚系列，包括 6-酰胺和 6-脲衍生物，它们的特点是对白色念珠菌具有杀菌活性，最小杀菌浓度 (MFC) 值 < 15 µM。6-酰胺衍生物对白色念珠菌表现出最高的杀菌活性，特别是化合物 1、5 和 6，其 MFC 值为 6.25-12.5 µM。该系列的化合物 1 和 5 对新兴病原体光滑念珠菌也具有杀菌活性 (MFC < 50 µM)。6-酰胺衍生物 1、2、5 和 6 以及 6-脲衍生物 10、12、13 和 15 也可以消除白色念珠菌生物膜。我们发现 6-脲衍生物 10、13 和 15 诱导白色念珠菌生物膜中内源性活性氧物质的积累。
