N,N′-diaryl-bishydrazones in a biphenyl platform: Broad spectrum antifungal agents

被引：12

作者：

Chandrika, Nishad Thamban ^{[1
]}

Dennis, Emily K. ^{[1
]}

Shrestha, Sanjib K. ^{[1
]}

Ngo, Huy X. ^{[1
]}

Green, Keith D. ^{[1
]}

Kwiatkowski, Stefan ^{[1
,2
]}

Deaciuc, Agripina Gabriela ^{[1
]}

Dwoskin, Linda P. ^{[1
]}

Watt, David S. ^{[2
,3
,4
]}

Garneau-Tsodikova, Sylvie ^{[1
]}

机构：

[1] Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA

[2] Univ Kentucky, Coll Pharm, Ctr Pharmaceut Res & Innovat, Lexington, KY 40536 USA

[3] Univ Kentucky, Coll Med, Dept Mol & Cellular Biochem, Lexington, KY 40536 USA

[4] Univ Kentucky, Lucille Parker Markey Canc Ctr, Lexington, KY 40536 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2019年 / 164卷

关键词：

Aspergillus sp; Candida albicans; Cytotoxicity; Hemolysis; hERG channel; Non-albicans Candida; AMPHIPHILIC AMINOGLYCOSIDE K20; DERIVATIVES; AZOLES; ANTIBACTERIAL; BIOACTIVITIES; VORICONAZOLE; KANAMYCIN; EBSELEN; ANALOGS;

D O I：

10.1016/j.ejmech.2018.12.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N,N'-Diaryl-bishydrazones of [1,1'-biphenyl]-3,4'-dicarboxaldehyde, [1,1'-biphenyl]-4,4'-dicarboxaldehyde, and 4,4'-bisacety1-1,1-biphenyl exhibited excellent antifungal activity against a broad spectrum of filamentous and non-filamentous fungi. These N,N'-diaryl-bishydrazones displayed no antibacterial activity in contrast to previously reported N,N'-diamidino-bishydrazones and N-amidino-N'-aryl-bishydrazones. The leading candidate, 4,4'-bis((E)-1-(2-(4-fluorophenyl)hydrazono)ethyl)-1,1'-biphenyl, displayed less hemolysis of murine red blood cells at concentrations at or below that of a control antifungal agent (voriconazole), was fungistatic in a time-kill study, and possessed no mammalian cytotoxicity and no toxicity with respect to hERG inhibition. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：273 / 281

页数：9

共 57 条

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