Synthesis, physiochemical property and antimicrobial activity of novel quaternary ammonium salts. (1st January 2018)

• Record Type: Journal Article
• Authors: Xie, Xianrui; Cong, Wei; Zhao, Feng; Li, Hongjuan; Xin, Wenyu; Hou, Guige; Wang, Chunhua
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 33:Number 1(2018)
• Page Start: 98
• Page End: 105
• Publication Date: 2018-01-01
• Subjects: 5-Phenyl-1, 3, 4-oxadiazole-2-thiol -- quaternary ammonium salts -- antibacterial activity -- antifungal activity -- cytotoxicity; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2017.1396456
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: Twenty-four novel 5-phenyl-1, 3, 4-oxadiazole-2-thiol (POT) analogues, benzo[ d ]oxazole-2-thiol, benzo[ d ]thiazole-2-thiol and 5-methyl-1, 3, 4-thiadiazole-2-thiol-substituted N, N -bis(2-hydroxyethyl) quaternary ammonium salts (QAS) (5a-d, 6a-d, 7a-d, 10a-d, 13a-d, 16a-d ) were prepared and characterised by FTIR, NMR and elemental analysis. Part of target compounds (5d, 6d, 7d, 10d, 13d, 16d ) displayed potent antimicrobial effect against ten common pathogens ( S. aureus, α-H-tococcus, β-H-tococcus, E. coli, P. aeruginosa, Proteus vulgaris, Canidia Albicans, Cytospora mandshurica, Physalospora piricola, Aspergillus niger ) and had relatively low cytotoxity against two human cell lines (HaCat and LO2). TEM and SEM images of E. coli and S. aureus morphologies treated with7d showed that the antibacterial mechanism might be the QAS fixing on cell wall surfaces and puncturing to result in the release of bacterial cytoplasm. This study provides new information of QAS, which could be used to design novel antimicrobial agents applied in clinic or agriculture. Graphical Abstract: