Biological evaluation and molecular modelling study of thiosemicarbazide derivatives as bacterial type IIA topoisomerases inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry
Agata PanethPiotr Paneth

Abstract

In the present article, we describe the inhibitory potency of nine thiosemicarbazide derivatives against bacterial type IIA topoisomerases, their antibacterial profile and molecular modelling evaluation. We found that one of the tested compounds, compound 7, significantly inhibits activity of Staphylococcus aureus DNA gyrase with an IC(50) below 15 μM. Besides, this compound displays antibacterial activity on reference Staphylococuss spp. and Enterococcus faecalis strains as well as clinical S. aureus isolates at non-cytotoxic concentrations in mammalian cells with MIC values ranging from 16 to 32 μg/mL thereby indicating, in some cases, equipotent or even more effective action than standard drugs such as vancomycin, ampicillin and nitrofurantoin. The computational studies showed that both molecular geometry and the electron density distribution have a great impact on antibacterial activity of thiosemicarbazide derivatives.

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Citations

Jul 23, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Veronica D'AngeloMarcello Locatelli
Jun 9, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Agata PanethPiotr Paneth
Nov 8, 2017·Current Medicinal Chemistry·Lanhua Yi, Xin Lü
Jun 21, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Katarzyna DziduchMonika Wujec
May 20, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Beata Chudzik-RządAgata Paneth
Jan 6, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Urszula KosikowskaAgata Paneth

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