<p>A series of pyridoxine-based tris-ammonium compounds was synthesized. Primary <i>in vitro</i> screening of antibacterial activity of the synthesized compounds against six reference bacterial strains revealed four compounds whose activity is comparable with clinically used antiseptics (benzalkonium chloride, miramistin, and chlorhexidine). Further in-depth <i>in vitro</i> studies of cytotoxicity and antibacterial activity against clinical bacterial strains indicated that the most active lead-compound <b>1a</b> is safer than benzalkonium chloride, miramistin, and chlorhexidine and is more active against both Gram-positive and Gram-negative clinical strains.</p>

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Synthesis and antibacterial activity of pyridoxine-based tris-ammonium compounds

  • N. V. Shtyrlin,
  • E. S. Bulatova,
  • S. V. Sapozhnikov,
  • M. N. Agafonova,
  • E. D. Kobylinskaya,
  • E. A. Ocherednyuk,
  • V. A. Burilov,
  • Yu. G. Shtyrlin

摘要

A series of pyridoxine-based tris-ammonium compounds was synthesized. Primary in vitro screening of antibacterial activity of the synthesized compounds against six reference bacterial strains revealed four compounds whose activity is comparable with clinically used antiseptics (benzalkonium chloride, miramistin, and chlorhexidine). Further in-depth in vitro studies of cytotoxicity and antibacterial activity against clinical bacterial strains indicated that the most active lead-compound 1a is safer than benzalkonium chloride, miramistin, and chlorhexidine and is more active against both Gram-positive and Gram-negative clinical strains.