CAGE ARYLSULFONAMIDES AND THEIR ANTIMICROBIAL PROPERTIES

Authors

  • Vitalii A. Palchykov Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University, Ukraine
  • Katerina V. Dil Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University, Ukraine
  • Nazar О. Manko Institute of Cell Biology of National Academy of Sciences of Ukraine, Ukraine
  • Nataliya S. Finiuk Institute of Cell Biology of National Academy of Sciences of Ukraine, Ukraine
  • Оlha Т. Novikevych Stepan Gzhytskyi National University of Veterinary Medicine and Biotechnologies Lviv, Ukraine
  • Nazariy T. Pokhodylo Stepan Gzhytskyi National University of Veterinary Medicine and Biotechnologies , Ukraine

DOI:

https://doi.org/10.15421/jchemtech.v30i1.246451

Keywords:

nitrobenzenesulfonamides; (aza)norbornane; 3-azabicyclo[3.2.1]oct-6-ene; cytotoxicity; SwissADME tool

Abstract

Arylsulfonamides bearing (aza)norbornane, 3-azabicyclo[3.2.1]oct-6-ene and related motifs were selected and evaluated for antimicrobial activity toward five key ESKAPE pathogenic bacteria, one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (ATCC 43300), four Gram‐negative bacteria, Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853) and antifungal activity towards two pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). One compound with 4-nitrobenzenesulfonamide motif demonstrated high activity towards methicillin‐resistant Staphylococcus aureus (ATCC 43300). The compound VP-4606 has low cytotoxicity towards pseudo-normal cells of HaCaT, Balb/c 3T3 lines, and mitogen-activated lymphocytes isolated from healthy adult peripheral blood of healthy donor up to 2.5 mM.

Author Biography

Vitalii A. Palchykov, Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University

Director Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University

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Published

2022-04-27