Abstract: 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.
Keywords: antifungal agents; Candida spp.; 2,6-disubstituted quinolines; reactive oxygen species; structure-activity relationships
This is an open access article distributed under the
Creative Commons Attribution License which permits unrestricted use, distribution,
and reproduction in any medium, provided the original work is properly cited.
Export to BibTeX
MDPI and ACS Style
Delattin, N.; Bardiot, D.; Marchand, A.; Chaltin, P.; De Brucker, K.; Cammue, B.P.A.; Thevissen, K. Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms. Molecules 2012, 17, 12243-12251.
Delattin N, Bardiot D, Marchand A, Chaltin P, De Brucker K, Cammue BPA, Thevissen K. Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms. Molecules. 2012; 17(10):12243-12251.
Delattin, Nicolas; Bardiot, Dorothée; Marchand, Arnaud; Chaltin, Patrick; De Brucker, Katrijn; Cammue, Bruno P. A.; Thevissen, Karin. 2012. "Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms." Molecules 17, no. 10: 12243-12251.