Publication details

Critical view on antimicrobial, antibiofilm and cytotoxic activities of quinazolin-4(3<i> H</i> )-one derived schiff bases and their Cu (II) complexes

Authors

PINDJAKOVA Dominika MASCARETTI Sarka HRICOVINIOVA Jana HOSEK Jan GREGOROVÁ Jana KOS Jiří CIZEK Alois HRICOVINIOVA Zuzana JAMPILEK Josef

Year of publication 2024
Type Article in Periodical
Magazine / Source Heliyon
MU Faculty or unit

Faculty of Medicine

Citation
Web https://www.sciencedirect.com/science/article/pii/S2405844024050825?via%3Dihub
Doi http://dx.doi.org/10.1016/j.heliyon.2024.e29051
Keywords Quinazolinones; Schiff bases; Cu(II) complexes; Antibacterial activity; Antibiofilm effect; Cytotoxicity
Description A series of nine 2,3-disubstituted-quinazolin-4(3 H )-one derived Schiff bases and their three Cu(II) complexes was prepared and tested for their antimicrobial activities against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis (VRE). All the substances were tested in vitro against Mycobacterium tuberculosis H 37 Ra ATCC 25177, M. kansasii DSM 44162 and M. smegmatis ATCC 700084. While anti-enterococcal and antimycobacterial activities were insignificant, 3-[( E )-(2-hydroxy-5-nitrobenzylidene)amino]-2-(2- hydroxy-5-nitrophenyl)-2,3-dihydroquinazolin-4(1 H )-one ( SB3 ) and its Cu(II) complex ( SB3 -Cu ) demonstrated bacteriostatic antistaphylococcal activity. In addition, both compounds, as well as the other two prepared complexes, showed antibiofilm activity, which resulted in a reduction of biofilm formation and eradication of mature S. aureus biofilm by 80% even at concentrations lower than the values of their minimum inhibitory concentrations. In addition, the compounds were tested for their cytotoxic effect on the human monocytic leukemia cell line THP-1. The antileukemic efficiency was improved by the preparation of Cu(II) complexes from the corresponding non-chelated Schiff base ligands.

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