1. Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones.
- Author
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Thamban Chandrika N, Dennis EK, Brubaker KR, Kwiatkowski S, Watt DS, and Garneau-Tsodikova S
- Subjects
- Animals, Antifungal Agents chemical synthesis, Antifungal Agents pharmacology, Biofilms drug effects, Candida drug effects, Candida physiology, Cell Line, Cell Survival drug effects, Drug Resistance, Microbial drug effects, Halogenation, Hemolysis drug effects, Humans, Hydrazones chemical synthesis, Hydrazones pharmacology, Mice, Microbial Sensitivity Tests, Structure-Activity Relationship, Voriconazole pharmacology, Antifungal Agents chemistry, Hydrazones chemistry
- Abstract
Fluorinated aryl- and heteroaryl-substituted monohydrazones displayed excellent broad-spectrum activity against various fungal strains, including a panel of clinically relevant Candida auris strains relative to a control antifungal agent, voriconazole (VRC). These monohydrazones displayed less hemolysis of murine red blood cells than that of VRC at the same concentrations, possessed fungicidal activity in a time-kill study, and exhibited no mammalian cell cytotoxicity. In addition, these monohydrazones prevented the formation of biofilms that otherwise block antibiotic effectiveness and did not trigger the development of resistance when exposed to C. auris AR Bank # 0390 over 15 passages., (© 2020 Wiley-VCH GmbH.)
- Published
- 2021
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