Synthesis and antibacterial activity of quaternary ammonium compounds with pentaerythritol and pyridoxine moieties
摘要
The synthesis of 28 quaternary bis-, tris-, and tetrakis-ammonium compounds based on pentaerythritol and pyridoxine was described. Primary in vitro screening of antibacterial activity against 11 reference bacterial strains revealed five lead compounds with minimal inhibitory concentration (MIC) against Gram-positive and Gram-negative bacteria of 1–32 and 4–32 µg mL−1, respectively, and activity comparable to that of commercial antiseptics (benzalkonium chloride, miramistin, and chlorhexidine). The in-depth in vitro studies of toxicity and antibacterial activity of the lead compounds against 19 clinical bacterial strains indicated that safety and activity of compounds 11a, 12a, and 17b against both Gram-positive (MIC 1–16 µg mL−1) and Gram-negative (MIC 1–32 µg mL−1) bacterial strains are comparable to those of benzalkonium chloride, miramistin, and chlorhexidine.