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Molecules 2012, 17(10), 12243-12251; doi:10.3390/molecules171012243
Article

Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms

1, 2, 2, 2,3, 1, 1,*  and 1
1 Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001, Heverlee, Belgium 2 CISTIM Leuven vzw, Minderbroedersstraat 12, B-3000, Leuven, Belgium 3 Centre for Drug Design and Discovery, Minderbroedersstraat 8a, B-3000, Leuven, Belgium
* Author to whom correspondence should be addressed.
Received: 13 September 2012 / Revised: 27 September 2012 / Accepted: 15 October 2012 / Published: 18 October 2012
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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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 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 (CC BY 3.0).

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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.

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