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广谱抗真菌药物：氟化芳基和杂芳基取代腙。

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

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA.

Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, Lexington, KY, 40536-0596, USA.

出版信息

ChemMedChem. 2021 Jan 8;16(1):124-133. doi: 10.1002/cmdc.202000626. Epub 2020 Oct 16.

DOI:10.1002/cmdc.202000626
PMID:33063957
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10898509/
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.

摘要

氟代芳基和杂芳基取代的单腙表现出对各种真菌菌株的优异广谱活性，包括一组临床相关的近平滑念珠菌菌株，相对于对照抗真菌药物伏立康唑（VRC）。与相同浓度的 VRC 相比，这些单腙对鼠红细胞的溶血作用较小，在时间杀伤研究中具有杀菌活性，并且对哺乳动物细胞没有细胞毒性。此外，这些单腙阻止了生物膜的形成，否则会阻止抗生素的有效性，并且在暴露于 C. auris AR Bank # 0390 超过 15 个传代时不会引发耐药性的发展。

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