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Identification of fungicidal 2,6-disubstituted quinolines with Candida antibiofilm activity

Journal Contribution - Journal Article

We 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) < 15 μM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 737, 742 and 744 characterized by MFC values of 6.25 - 12.5 μM. Compounds 737 and 742 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata (MFC < 50 μM). The 6-amide derivatives 737, 738, 742, and 744 and the 6-urea derivatives 798, 803, 804 and 807 could eradicate C. albicans biofilms. We found that the 6-urea derivatives 798, 804, and 807 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms.
Journal: Molecules
ISSN: 1420-3049
Issue: 10
Volume: 17
Pages: 12243 - 12251
Publication year:2012
Accessibility:Open