A.E.Arbuzov Institute of Organic and Physical Chemistry, FRC, Kazan Scientific Center of RAS, 8 Arbuzov Str., Kazan, 420088, Russian Federation.
Kazan National Research Technological University, 68 K. Marx Str., Kazan, 420015, Russian Federation.
Chem Biodivers. 2020 May;17(5):e2000147. doi: 10.1002/cbdv.202000147. Epub 2020 Apr 29.
The increase in the resistance of pathogens, in particular Staphylococcus aureus, to the action of antibiotics necessitates the search for new readily available and non-toxic drugs. In solving this problem, phenolic acylhydrazones have high potential. In this communication, the synthesis of quaternary ammonium compounds containing a differently substituted phenolic moiety has been performed. An initial study of antimicrobial activity showed that these compounds are highly selective against S. aureus and B. cereus. The highest activity (MIC 2.0 μm) was shown by hydrazones containing a catechol fragment. These compounds are more than 3-fold more active against S. aureus and 3-10-fold more active against B. cereus than norfloxacin. Low hemolytic and high antioxidant activities of all new compounds were also established.
病原体（尤其是金黄色葡萄球菌）对抗生素作用的耐药性不断增加，这就需要寻找新的易得且无毒的药物。在解决这个问题的过程中，酚酰腙类化合物具有很大的潜力。在本通讯中，已经完成了含有不同取代酚部分的季铵化合物的合成。抗菌活性的初步研究表明，这些化合物对金黄色葡萄球菌和蜡状芽孢杆菌具有高度的选择性。含有儿茶酚片段的腙类化合物表现出最高的活性（MIC 2.0 μm）。这些化合物对金黄色葡萄球菌的活性比诺氟沙星高 3 倍以上，对蜡状芽孢杆菌的活性高 3-10 倍。所有新化合物的溶血活性低、抗氧化活性高。
