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双吗啉三嗪季铵盐的合成与抗菌评价。

Synthesis and Antimicrobial Evaluation of Bis-morpholine Triazine Quaternary Ammonium Salts.

机构信息

Dipartimento di Scienze Molecolari e Nanosistemi, Università Ca' Foscari di Venezia, Via Torino 155, 30172, Venezia Mestre, Italy.

Brenta S.r.l. - Nine trees group, Viale Milano 26, 36075, Montecchio Maggiore, Vicenza, Italy.

出版信息

ChemMedChem. 2021 Oct 15;16(20):3172-3176. doi: 10.1002/cmdc.202100409. Epub 2021 Jul 29.

Abstract

Efficient, environmentally and economically sustainable, and nontoxic antibacterial products are of global relevance in the fight against microorganism contamination. In this work, an easy and straightforward method for the synthesis of bis-morpholino triazine quaternary ammonium salts (bis-mTQAS) is reported, starting from 2,4,6-trichloro-1,3,5-triazine or 2,4-dichloro-6-methoxy-1,3,5-triazine and various N-alkylmorpholines. Bis-mTQAS were tested as antimicrobials against Gram-negative and Gram-positive bacterial strains. The best-performing bis-mTQAS were found to achieve total disinfection against Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 25922 at 50 and 400 μg/mL, respectively. Distinctively, bis-mTQAS with the highest antimicrobial efficiency had lowest cytotoxicity.

摘要

高效、环保、经济可持续且无毒的抗菌产品在对抗微生物污染方面具有全球意义。在这项工作中,报道了一种从 2,4,6-三氯-1,3,5-三嗪或 2,4-二氯-6-甲氧基-1,3,5-三嗪和各种 N-烷基吗啉出发合成双吗啉三嗪季铵盐(bis-mTQAS)的简单方法。将双-mTQAS 作为抗菌剂测试对革兰氏阴性和革兰氏阳性细菌菌株的作用。结果发现,表现最好的双-mTQAS 在 50 和 400μg/mL 时分别对金黄色葡萄球菌 ATCC 25923 和大肠杆菌 ATCC 25922 实现完全消毒。值得注意的是,抗菌效率最高的双-mTQAS 具有最低的细胞毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/abf9/8596621/0e0e843d450c/CMDC-16-3172-g003.jpg

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