Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors
A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-09-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/18/9709 |
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| author | Dariusz Karcz Karolina Starzak Ewa Ciszkowicz Katarzyna Lecka-Szlachta Daniel Kamiński Bernadette Creaven Hollie Jenkins Piotr Radomski Anna Miłoś Lidia Ślusarczyk Arkadiusz Matwijczuk |
| author_facet | Dariusz Karcz Karolina Starzak Ewa Ciszkowicz Katarzyna Lecka-Szlachta Daniel Kamiński Bernadette Creaven Hollie Jenkins Piotr Radomski Anna Miłoś Lidia Ślusarczyk Arkadiusz Matwijczuk |
| author_sort | Dariusz Karcz |
| collection | DOAJ |
| description | A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (<i>Staphylococcus aureus</i>, <i>Staphylococcus epidermidis</i>) and Gram-negative (<i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity |
| first_indexed | 2024-03-10T07:37:19Z |
| format | Article |
| id | doaj.art-fdf44386e9674ea5923a7286cd57d3d6 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T07:37:19Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-fdf44386e9674ea5923a7286cd57d3d62023-11-22T13:26:38ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-09-012218970910.3390/ijms22189709Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase InhibitorsDariusz Karcz0Karolina Starzak1Ewa Ciszkowicz2Katarzyna Lecka-Szlachta3Daniel Kamiński4Bernadette Creaven5Hollie Jenkins6Piotr Radomski7Anna Miłoś8Lidia Ślusarczyk9Arkadiusz Matwijczuk10Department of Chemical Technology and Environmental Analytics (C1), Faculty of Chemical Engineering and Technology, Cracow University of Technology, 31-155 Kraków, PolandDepartment of Chemical Technology and Environmental Analytics (C1), Faculty of Chemical Engineering and Technology, Cracow University of Technology, 31-155 Kraków, PolandDepartment of Biotechnology and Bioinformatics, Faculty of Chemistry, Rzeszow University of Technology, 35-959 Rzeszów, PolandDepartment of Biotechnology and Bioinformatics, Faculty of Chemistry, Rzeszow University of Technology, 35-959 Rzeszów, PolandDepartment of General and Coordination Chemistry and Crystallography, Institute of Chemical Sciences, Maria Curie-Sklodowska University in Lublin, 20-031 Lublin, PolandSchool of Chemical and Pharmaceutical Sciences, Technological University Dublin, Central Quad, D07 ADY7 Grangegorman, IrelandDepartment of Applied Science, Technological University Dublin, D24 FKT9 Tallaght, IrelandDepartment of Chemical Technology and Environmental Analytics (C1), Faculty of Chemical Engineering and Technology, Cracow University of Technology, 31-155 Kraków, PolandDepartment of Biotechnology and Bioinformatics, Faculty of Chemistry, Doctoral School of Engineering and Technical Sciences at the Rzeszow University of Technology, 35-959 Rzeszow, PolandDepartment of Biophysics, University of Life Sciences in Lublin, 20-950 Lublin, PolandDepartment of Biophysics, University of Life Sciences in Lublin, 20-950 Lublin, PolandA series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (<i>Staphylococcus aureus</i>, <i>Staphylococcus epidermidis</i>) and Gram-negative (<i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activityhttps://www.mdpi.com/1422-0067/22/18/9709coumarinthiadiazolehybridscomplexesantimicrobialantibacterial activity |
| spellingShingle | Dariusz Karcz Karolina Starzak Ewa Ciszkowicz Katarzyna Lecka-Szlachta Daniel Kamiński Bernadette Creaven Hollie Jenkins Piotr Radomski Anna Miłoś Lidia Ślusarczyk Arkadiusz Matwijczuk Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors International Journal of Molecular Sciences coumarin thiadiazole hybrids complexes antimicrobial antibacterial activity |
| title | Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
| title_full | Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
| title_fullStr | Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
| title_full_unstemmed | Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
| title_short | Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
| title_sort | novel coumarin thiadiazole hybrids and their cu ii and zn ii complexes as potential antimicrobial agents and acetylcholinesterase inhibitors |
| topic | coumarin thiadiazole hybrids complexes antimicrobial antibacterial activity |
| url | https://www.mdpi.com/1422-0067/22/18/9709 |
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