Tag Archives: antimicrobial

Synthesis of the novel cage amides and imides and evaluation of their antibacterial and antifungal activity

V. Palchykov1*, A. Gaponov1, N. Manko2,3, N. Finiuk2,
О. Novikevych4, O. Gromyko3, R. Stoika2, N. Pokhodylo3,4*

1Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University, Ukraine;
2Institute of Cell Biology of National Academy of Sciences of Ukraine, Lviv;
3Ivan Franko National University of Lviv, Ukraine;
4Stepan Gzhytskyi National University of Veterinary Medicine and Biotechnologies Lviv, Ukraine;
*e-mail: pokhodylo@gmail.com; palchikoff82@gmail.com

Received: 28 December 2021; Revised: 29 June 2022;
Accepted: 29 September 2022; Available on-line: 06 October 2022

Cage amides and imides bearing bicyclo[2.2.1]- and bicyclo[2.2.2]-subunits were synthesized and evaluated both 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 pneumoniae (ATCC 700603), Acinetobacter baumannii (ATCC 19606) and Pseudomonas aeruginosa (ATCC 27853) and for antifungal activity towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). Compound VP-4539 with bicyclo[2.2.2]octene motif demonstrated the highest cytotoxic activity towards C. neoformans, while human keratinocytes of HaCaT line, murine fibroblasts of Balb/c 3T3 line and mitogen-activated lymphocytes of peripheral human blood were found to be tolerant to its action. VP-4539 compound did not intercalate into salmon sperm DNA indicating that its cytotoxicity is not related to intercalation into nucleic acid.

New dinuclear cyanido complexes with amine alcohol ligand: synthesis, characterization and biotechnological application potential

N. Korkmaz1*, Ş. A. Korkmaz2, Y. Ceylan3,
R. İmamoğlu3, A. S. Bülbül4, A. Karadağ5

1Department of Basic Sciences and Health, Hemp Institute, Yozgat Bozok University, Yozgat, Turkey;
2Department of Chemistry and Chemical Processing Technologies, Tunceli Vocational School, Munzur University, Tunceli, Turkey;
3Faculty of Science, Department of Molecular Biology and Genetics, Bartın University, Bartın, Turkey;
4Department of Biology, Faculty of Science and Arts, Kahramanmaraş Sütçü İmam University, Kahramanmaraş, Turkey;
5Department of Chemistry, Faculty of Arts and Sciences, Yozgat Bozok University, Yozgat, Turkey;
*e-mail: nesrinokumus@gmail.com

Received: 14 September 2021; Accepted: 21 January 2022

In this study, the cyanido complexes given by the formula [Ni(Abut)Ni(CN)4]·8H2O (C1), [Cu(Abut)2Ni(CN)4]·7H2O (C2), [Zn(Abut)Ni(CN)4]·8H2O (C3) and [Cd(Abut)Ni(CN)4]·7H2O (C4) were obtained by microwave synthesis method. The powder forms of the complexes were characterized by elemental, FT-IR spectroscopy, and thermal analysis. And also antibacterial, antibiofilm and anticancer activities were investigated. The splitting stretching bands of cyanido groups in the FT-IR spectra of C1-C4 indicated the assets of terminal and end cyanido groups. The antibacterial activities of C1-C4 were tested with nine Gram negative and six Gram positive bacteria. The most efficient antibacterial activity of complexes was observed at 1000 µg/ml-1 concentration. Anticancer activity was tested using HeLa cell line and MTT test. The studied cyanide complexes have been shown to decrease the viability of HeLa cells with IC50 values 14.86, 6.5, 7.2 and 19.2 µg/ml for C1, C2, C3 and C4 complex, respectively.

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

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.