Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Akad. Arbuzov st. 8, 420088 Kazan, Russia.
Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 119991 Moscow, Russia.
Int J Mol Sci. 2024 Oct 17;25(20):11130. doi: 10.3390/ijms252011130.
A series of new isatin-3-hydrazones bearing different ammonium fragments was synthesized by a simple and easy work-up reaction of Girard's reagents analogs with 1-(3,5-di--butyl-4-hydroxybenzyl)isatin. All derivatives have been shown to have antioxidant properties. In terms of bactericidal activity against gram-positive bacteria, including methicillin-resistant strains of , the best compounds are , , and , bearing octyl, acetal, and brucine ammonium centers, respectively. In addition, brucine and quinine derivatives , and exhibit platelet antiaggregation activity at the level of acetylsalicylic acid, and this series of isatin derivatives does not adversely affect the hemostasis system as a whole. Thus, all the obtained results can lay the groundwork for future pharmaceutical developments for the creation of effective antibacterial drugs with reduced systemic toxicity due to the presence of antioxidant properties.
一系列新的含不同铵片段的靛红-3-腙是通过简单易行的反应，由 1-(3,5-二-叔丁基-4-羟基苄基)靛红与吉拉尔试剂类似物反应合成的。所有的衍生物都表现出抗氧化特性。在抗革兰氏阳性菌的杀菌活性方面，包括耐甲氧西林的 ，最好的化合物是 、 、 和 ，分别带有辛基、缩醛和金鸡纳铵中心。此外，金鸡纳和奎宁衍生物 、 和 具有与乙酰水杨酸相当的血小板抗聚集活性，而这一系列的靛红衍生物对整个止血系统没有不良影响。因此，所有获得的结果可以为未来的药物开发奠定基础，以创造具有抗氧化特性的有效抗菌药物，降低系统毒性。
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