ADMET and DMPK (Jan 2022)

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

  • Andrei Bogdanov,
  • Olga Tsivileva,
  • Alexandra Voloshina,
  • Anna Lyubina,
  • Syumbelya Amerhanova,
  • Ekaterina Burtceva,
  • Sergey Bukharov,
  • Alexander Samorodov,
  • Valentin Pavlov

DOI
https://doi.org/10.5599/admet.1179

Abstract

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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.