Ammonium‐Charged Sterically Hindered Phenols with Antioxidant and Selective Anti‐Gram‐Positive Bacterial Activity,Chemistry & Biodiversity

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Ammonium‐Charged Sterically Hindered Phenols with Antioxidant and Selective Anti‐Gram‐Positive Bacterial Activity
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-04-29 , DOI: 10.1002/cbdv.202000147
Andrei V Bogdanov ₁ , Kamilla R Iskhakova ₂ , Alexandra D Voloshina ₁ , Anastasia S Sapunova ₁ , Natalia V Kulik ₁ , Natalia V Terekhova ₁ , Maxim V Arsenyev ₃ , Guzel K Ziyatdinova ₄ , Sergey V Bukharov ₂

Affiliation

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.

中文翻译：

具有抗氧化和选择性抗革兰氏阳性细菌活性的带铵电荷的位阻酚

病原体（尤其是金黄色葡萄球菌）对抗生素作用的耐药性增加，需要寻找新的现成且无毒的药物。在解决这个问题上，酚酰腙具有很大的潜力。在此通讯中，已进行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选择性。含有儿茶酚片段的腙显示最高活性 (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，对蜡样芽孢杆菌的活性高 3-10 倍。还确定了所有新化合物的低溶血性和高抗氧化活性。

更新日期：2020-04-29

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