Details

Autor(en) / Beteiligte

• Thamban Chandrika, Nishad
• Dennis, Emily K.
• Shrestha, Sanjib K.
• Ngo, Huy X.
• Green, Keith D.
• Kwiatkowski, Stefan
• Deaciuc, Agripina Gabriela
• Dwoskin, Linda P.
• Watt, David S.
• Garneau-Tsodikova, Sylvie

Titel

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

Ist Teil von

• European journal of medicinal chemistry, 2019-02, Vol.164, p.273-281

Ort / Verlag

France: Elsevier Masson SAS

Erscheinungsjahr

2019

Quelle

MEDLINE

Beschreibungen/Notizen

• N,N′-Diaryl-bishydrazones of [1,1′-biphenyl]-3,4′-dicarboxaldehyde, [1,1′-biphenyl]-4,4′-dicarboxaldehyde, and 4,4′-bisacetyl-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. [Display omitted] •Novel N,N′-diaryl-bishydrazones display broad spectrum antifungal activity against various yeast and filamentous fungi.•The most active N,N'-diaryl-bishydrazones display low hemolysis of mRBCs and no toxicity with respect to hERG inhibition.•The most active N,N′-diaryl-bishydrazone display activity against pre-formed biofilms of C. albicans.