Bogdanov Andrei, Tsivileva Olga, Voloshina Alexandra, Lyubina Anna, Amerhanova Syumbelya, Burtceva Ekaterina, Bukharov Sergey, Samorodov Alexander, Pavlov Valentin
Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of RAS, Kazan, 420088, Russian Federation.
Institute of Biochemistry and Physiology of Plants and Microorganisms, Saratov Scientific Centre of the Russian Academy of Sciences, Saratov 410049, Russian Federation.
ADMET DMPK. 2022 Jan 12;10(2):163-179. doi: 10.5599/admet.1179. eCollection 2022.
A series of biorelevant triethylammonium isatin hydrazones containing various substituents in the aromatic fragment have been synthesized. Their structure and composition were confirmed by NMR- and IR-spectroscopies, mass-spectrometry and elemental analysis. It was found that some representatives show activity against and higher or at the level of norfloxacin, including methicillin-resistant strains. The study also showed low hemo- and cytotoxicity (Chang Liver) and high antiaggregatory and anticoagulant activity of these compounds. The high potential of new ammonium isatin-3-acylhydrazones in the search for antimicrobial activity against phytopathogens of bacterial and fungal nature has been shown for the first time.
已经合成了一系列在芳香片段中含有各种取代基的具有生物相关性的三乙铵异吲哚酮腙。通过核磁共振光谱、红外光谱、质谱和元素分析确定了它们的结构和组成。发现一些代表物对[具体细菌名称1]和[具体细菌名称2]具有活性，且活性高于或与诺氟沙星相当，包括耐甲氧西林的[具体细菌名称1]菌株。该研究还表明这些化合物具有低血液毒性和细胞毒性（Chang Liver）以及高抗聚集和抗凝活性。首次展示了新型铵异吲哚酮-3-酰腙在寻找针对细菌和真菌性质的植物病原体的抗菌活性方面的巨大潜力。
