Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms

Autor: Albina G. Malanyeva, Marsel R. Garipov, Konstantin V. Balakin, Alina E. Sabirova, Svetlana A. Lisovskaya, Elena V. Nikitina, Yurii G. Shtyrlin, Alfia G. Iksanova, A. M. Aimaletdinov, Airat R. Kayumov, Roman S. Pavelyev, Oksana V. Bondar
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Journal of Chemistry, Vol 2017 (2017)
ISSN: 2090-9071
2090-9063
Popis: Two novel quaternary ammonium salts, bis-triazolium derivatives of fluconazole and pyridoxine, were synthesized by reaction of fluconazole with pyridoxine-based synthetic intermediates. The leading compound demonstrated pronounced antimycotic and antibacterialin vitroactivity, comparable to or exceeding that of the reference antifungal (fluconazole, terbinafine) and antibacterial/antiseptic (miramistin, benzalkonium chloride) agents. In contrast to many antimicrobials, the leading compound was also active against biofilm-embedded staphylococci andEscherichia coli. While no biofilm structure destruction occurred, all compounds were able to diffuse into the matrix and reduce the number of colony-forming units by three orders of magnitude at 16 × MBC. The leading compound was significantly less toxic than miramistin and benzalkonium chloride and more toxic than the reference antifungal drugs. The obtained results make the described chemotype a promising starting point for the development of new broad-spectrum antimicrobial therapies with powerful effect on fungal and bacterial pathogens including their biofilm-embedded forms.
Databáze: OpenAIRE
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