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Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones.
- Source :
-
ChemMedChem [ChemMedChem] 2021 Jan 08; Vol. 16 (1), pp. 124-133. Date of Electronic Publication: 2020 Oct 16. - Publication Year :
- 2021
-
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.<br /> (© 2020 Wiley-VCH GmbH.)
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 16
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 33063957
- Full Text :
- https://doi.org/10.1002/cmdc.202000626