Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms
Joint Authors
Kayumov, Airat R.
Shtyrlin, Yurii G.
Bondar, Oksana V.
Garipov, Marsel R.
Pavelyev, Roman S.
Lisovskaya, Svetlana A.
Nikitina, Elena V.
Sabirova, Alina E.
Malanyeva, Albina G.
Aimaletdinov, Alexander M.
Iksanova, Alfia G.
Balakin, Konstantin V.
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-15, 15 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-12-27
Country of Publication
Egypt
No. of Pages
15
Main Subjects
Abstract EN
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 antibacterial in vitro activity, 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 and Escherichia 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.
American Psychological Association (APA)
Garipov, Marsel R.& Pavelyev, Roman S.& Lisovskaya, Svetlana A.& Nikitina, Elena V.& Kayumov, Airat R.& Sabirova, Alina E.…[et al.]. 2017. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms. Journal of Chemistry،Vol. 2017, no. 2017, pp.1-15.
https://search.emarefa.net/detail/BIM-1171895
Modern Language Association (MLA)
Garipov, Marsel R.…[et al.]. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms. Journal of Chemistry No. 2017 (2017), pp.1-15.
https://search.emarefa.net/detail/BIM-1171895
American Medical Association (AMA)
Garipov, Marsel R.& Pavelyev, Roman S.& Lisovskaya, Svetlana A.& Nikitina, Elena V.& Kayumov, Airat R.& Sabirova, Alina E.…[et al.]. Fluconazole-Pyridoxine Bis-Triazolium Compounds with Potent Activity against Pathogenic Bacteria and Fungi Including Their Biofilm-Embedded Forms. Journal of Chemistry. 2017. Vol. 2017, no. 2017, pp.1-15.
https://search.emarefa.net/detail/BIM-1171895
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1171895