Next Article in Journal
First Example of a Lipophilic Porphyrin-Cardanol Hybrid Embedded in a Cardanol-Based Micellar Nanodispersion
Next Article in Special Issue
Antimicrobial Peptides for Therapeutic Applications: A Review
Previous Article in Journal
Solvent-Free Synthesis of Modified Pectin Compounds Promoted by Microwave Irradiation
Previous Article in Special Issue
Synthesis and Antibacterial Activities of Amphiphilic Neomycin B-based Bilipid Conjugates and Fluorinated Neomycin B-based Lipids
Article Menu

Export Article

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

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

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)
View Full-Text   |   Download PDF [192 KB, uploaded 18 June 2014]   |  

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
Figures

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

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.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top