isatin-3-腙三乙基胺的合成及多种生物活性分析

IF 3.4 Q2 CHEMISTRY, MEDICINAL

ADMET and DMPK Pub Date : 2022-01-12 DOI:10.5599/admet.1179

A. Bogdanov, O. Tsivileva, A. Voloshina, A. Lyubina, S. Amerhanova, Ekaterina Burtceva, S. Bukharov, Alexander V. Samorodov, V. Pavlov

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引用次数: 4

摘要

合成了一系列具有生物相关性的含有不同取代基的isatin三乙基铵腙。它们的结构和组成经核磁共振、红外光谱、质谱和元素分析证实。发现部分代表对金黄色葡萄球菌和蜡样芽孢杆菌的活性高于或等于诺氟沙星水平，包括耐甲氧西林金黄色葡萄球菌菌株。该研究还表明，这些化合物具有低的血液和细胞毒性(长肝)和高的抗聚集和抗凝血活性。新的isatin-3-酰基腙在寻找对细菌和真菌性质的植物病原体的抗菌活性方面具有很高的潜力。

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Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones

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 Staphylococcus aureus and Bacillus cereus higher or at the level of norfloxacin, including methicillin-resistant Staphylococcus aureus 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.

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来源期刊

ADMET and DMPK Multiple-

CiteScore

4.40

自引率

0.00%

发文量

审稿时长

4 weeks

期刊介绍： ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study