1. In vitro antifungal and antibiofilm activities of halogenated quinoline analogues against Candida albicans and Cryptococcus neoformans.
- Author
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Zuo R, Garrison AT, Basak A, Zhang P, Huigens RW 3rd, and Ding Y
- Subjects
- Candida albicans physiology, Cryptococcus neoformans physiology, Halogenation, Humans, Microbial Sensitivity Tests, Antifungal Agents chemistry, Antifungal Agents pharmacology, Biofilms drug effects, Candida albicans drug effects, Cryptococcus neoformans drug effects, Quinolines chemistry, Quinolines pharmacology
- Abstract
With the increasing prevalence of fungal infections coupled with emerging drug resistance, there is an urgent need for new and effective antifungal agents. Here we report the antifungal activities of 19 diverse halogenated quinoline (HQ) small molecules against Candida albicans and Cryptococcus neoformans. Four HQ analogues inhibited C. albicans growth with a minimum inhibitory concentration (MIC) of 100 nM, whilst 16 analogues effectively inhibited C. neoformans at MICs of 50-780 nM. Remarkably, two HQ analogues eradicated mature C. albicans and C. neoformans biofilms [minimum biofilm eradication concentration (MBEC) = 6.25-62.5 µM]. Several active HQs were found to penetrate into fungal cells, whilst one inactive analogue was unable to, suggesting that HQs elicit their antifungal activities through an intracellular mode of action. HQs are a promising class of small molecules that may be useful in future antifungal treatments., (Copyright © 2016 Elsevier B.V. and International Society of Chemotherapy. All rights reserved.)
- Published
- 2016
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