Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones

Nishad Thamban Chandrika, Emily K. Dennis, Katelyn R. Brubaker, Stefan Kwiatkowski, David S. Watt, Sylvie Garneau-Tsodikova

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

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.

Original languageEnglish
Pages (from-to)124-133
Number of pages10
JournalChemMedChem
Volume16
Issue number1
DOIs
StatePublished - Jan 8 2021

Bibliographical note

Publisher Copyright:
© 2020 Wiley-VCH GmbH

Keywords

  • Biofilm
  • Candida auris
  • Cytotoxicity
  • Drug resistance
  • Hemolysis
  • Monohydrazones

ASJC Scopus subject areas

  • Drug Discovery
  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine
  • Biochemistry
  • Pharmacology
  • Organic Chemistry

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