<p>Successive condensation of pentaerythritol with 4-formylpyridine and 2,5-diformylfuran yielded a hybrid platform containing two pyridine and two pentaerythritol fragments and one furan fragment. <i>N</i>-Alkylation of this platform with alkyl iodides led to new bis-quaternary ammonium compounds. An assessment of the bacteriostatic and bactericidal potential of the obtained compounds against reference and clinical strains of ESKAPE pathogens, as well as yeast-like fungus <i>Candida albicans</i>, showed their ability to inhibit the growth and destroy mature biofilms of gram-positive and gram-negative bacteria and fungi. When comparing the activity of the synthesized compounds with known antiseptics (octenidine dihydrochloride and cetylpyridinium chloride), it was found that they are effective against various strains of <i>S. aureus</i>, <i>E. coli</i>, <i>K. pneumoniae</i>, <i>P. aeruginosa</i> and <i>C. albicans</i>.</p>

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Synthesis and antibacterial activity of new bis-quaternary ammonium compounds based on 2,5-diformylfuran and pentaerythritol

  • E. A. Saverina,
  • N. A. Frolov,
  • A. A. Tyutin,
  • E. A. Lantsova,
  • E. V. Detusheva,
  • E. Son,
  • A. N. Vereshchagin

摘要

Successive condensation of pentaerythritol with 4-formylpyridine and 2,5-diformylfuran yielded a hybrid platform containing two pyridine and two pentaerythritol fragments and one furan fragment. N-Alkylation of this platform with alkyl iodides led to new bis-quaternary ammonium compounds. An assessment of the bacteriostatic and bactericidal potential of the obtained compounds against reference and clinical strains of ESKAPE pathogens, as well as yeast-like fungus Candida albicans, showed their ability to inhibit the growth and destroy mature biofilms of gram-positive and gram-negative bacteria and fungi. When comparing the activity of the synthesized compounds with known antiseptics (octenidine dihydrochloride and cetylpyridinium chloride), it was found that they are effective against various strains of S. aureus, E. coli, K. pneumoniae, P. aeruginosa and C. albicans.