Isatin derivatives bearing a fluorine atom. Part 1: Synthesis, hemotoxicity and antimicrobial activity evaluation of fluoro-benzylated water-soluble pyridinium isatin-3-acylhydrazones
[Display omitted] •1-Fluorobenzylated isatins and water-soluble pyridinium isatin-3-acylhydrazones were synthesized.•Pyridinium isatin-3-acylhydrazones exhibit low hemotoxicity.•Antimicrobial activity of the novel compounds was studied.•Compounds containing a 2-fluoro-6-chlorobenzyl fragment showed...
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Veröffentlicht in: | Journal of fluorine chemistry 2019-11, Vol.227, p.109345, Article 109345 |
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Hauptverfasser: | , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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•1-Fluorobenzylated isatins and water-soluble pyridinium isatin-3-acylhydrazones were synthesized.•Pyridinium isatin-3-acylhydrazones exhibit low hemotoxicity.•Antimicrobial activity of the novel compounds was studied.•Compounds containing a 2-fluoro-6-chlorobenzyl fragment showed the best activity against S. aureus.
A series of 1-fluorobenzylated isatins and water-soluble pyridinium isatin-3-acylhydrazones on their base were obtained. The biological evaluation of novel hydrazones showed a significant dependence of their antimicrobial activity on the position of fluorine atom in benzyl substituent. The best activity showed compounds containing a 2-fluoro-6-chlorobenzyl fragment with selective action against S. aureus. The absence of hemotoxicity of both fluorine-containing products and their some non-fluorinated analogues was shown. |
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ISSN: | 0022-1139 1873-3328 |
DOI: | 10.1016/j.jfluchem.2019.109345 |