Ukr.Biochem.J. 2022; Volume 94, Issue 1, Jan-Feb, pp. 64-74

doi: https://doi.org/10.15407/ubj94.01.064

2-Amino-4,6,7,8-tetrahydrothiopyrano[3,2-b]pyran-3-carbonitrile 5,5-dioxide VP-4535 as an antimicrobial agent selective toward methicillin‐resistant Staphylococcus aureus

02.05.2022   Uncategorized   No comments

V. Palchykov1*, N. Manko2, N. Finiuk2, N. Pokhodylo3*

1Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University, Dnipro, Ukraine;
2Institute of Cell Biology, National Academy of Sciences of Ukraine, Lviv, Ukraine;
3Ivan Franko National University of Lviv, Lviv, Ukraine;
*e-mail: pokhodylo@gmail.com; palchikoff82@gmail.com

Received: 01 August 2021; Accepted: 21 January 2022

The antibacterial activity of 2-amino-4,6,7,8-tetrahydrothiopyrano[3,2-b]pyran-3-carbonitrile 5,5-dioxide toward five key ESKAPE pathogenic bacteria, methicillin‐resistant Staphylococcus aureus (ATCC 43300), Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853) was evaluated. The antifungal activity was studied­ towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (ATCC 208821). Compound VP-4535 bearing 5-methylindolin-2-one motif possessed the highest antibacterial activity and excellent selectivity toward methicillin‐resistant Staphylococcus aureus but was inactive against non-resistant Staphylococcus aureus strain. The compound in therapeutic concentration was safe to human red blood cells, human lymphocytes, HaCaT, Balb/c 3T3 and HEK-293 cells.

Keywords: , , , , ,

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