Kazan (Volga region) Federal University, KFU
KAZAN
FEDERAL UNIVERSITY
 
TARGETING PATHOGENIC FUNGI, BACTERIA AND FUNGAL-BACTERIAL BIOFILMS BY NEWLY SYNTHESIZED QUATERNARY AMMONIUM DERIVATIVE OF PYRIDOXINE AND TERBINAFINE WITH DUAL ACTION PROFILE
Form of presentationArticles in international journals and collections
Year of publication2020
Языканглийский
  • Bogachev Mikhail Igorevich, author
  • Kayumov Ayrat Rashitovich, author
  • Laykov Aleksandr Vladimirovich, author
  • Pavelev Roman Sergeevich, author
  • Bibliographic description in the original language Garipov M.R, Sabirova A.E, Pavelyev R.S, Targeting pathogenic fungi, bacteria and fungal-bacterial biofilms by newly synthesized quaternary ammonium derivative of pyridoxine and terbinafine with dual action profile//Bioorganic Chemistry. - 2020. - Vol.104, Is.. - Art. № 104306.
    Annotation Many pathogenic bacteria and microscopic fungi form rigid polymicrobial biofilms this way enhancing their resistant to treatment. A series of novel pyridoxine-based quaternary ammonium derivatives of terbinafine characterized by both antifungal and antibacterial activities was designed. The leading compound named KFU-127 exhibits promising antifungal and antibacterial activities against various bacteria and micromycetes in both planktonic and biofilm-embedded forms demonstrating MIC values comparable with those of conventional antifungals and antimicrobials. Similar to other antiseptics like benzalkonium chloride and miramistin, KFU-127 is considerably toxic for eukaryotic cells that limits is application to topical treatment options. On the other hand, KFU-127 reduces the number of viable biofilm-embedded bacteria and C. albicans by 3 orders of magnitude at concentrations 2–4 times lower than those of reference drugs and successfully eradicates S. aureus-C. albicans mixed biofilms. The mechanism of antimicrobial action of KFU-127 is bimodal including both membrane integrity damage and pyridoxal-dependent enzymes targeting. We expect that this bilateral mechanism would result in lower rates of resistance development in both fungal and bacterial pathogens. Taken together, our data suggest KFU-127 as a new promising broad spectrum topical antimicrobial capable of one-shot targeting of bacterial and fungal-bacterial biofilms.
    Keywords Antifungals Antimicrobials Quaternary ammonium compounds (QAC) Terbinafine Pyridoxine Biofilms
    The name of the journal Bioorganic Chemistry
    URL https://www.scopus.com/inward/record.uri?eid=2-s2.0-85091800881&doi=10.1016%2fj.bioorg.2020.104306&partnerID=40&md5=5d45a12b6fa0e7db459d297ae4da4557
    Please use this ID to quote from or refer to the card https://repository.kpfu.ru/eng/?p_id=240205&p_lang=2

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