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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...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8471537/ https://www.ncbi.nlm.nih.gov/pubmed/34575894 http://dx.doi.org/10.3390/ijms22189709 |
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author | Karcz, Dariusz Starzak, Karolina Ciszkowicz, Ewa Lecka-Szlachta, Katarzyna Kamiński, Daniel Creaven, Bernadette Jenkins, Hollie Radomski, Piotr Miłoś, Anna Ślusarczyk, Lidia Matwijczuk, Arkadiusz |
author_facet | Karcz, Dariusz Starzak, Karolina Ciszkowicz, Ewa Lecka-Szlachta, Katarzyna Kamiński, Daniel Creaven, Bernadette Jenkins, Hollie Radomski, Piotr Miłoś, Anna Ślusarczyk, Lidia Matwijczuk, Arkadiusz |
author_sort | Karcz, Dariusz |
collection | PubMed |
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 (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) 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 |
format | Online Article Text |
id | pubmed-8471537 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-84715372021-09-28 Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors Karcz, Dariusz Starzak, Karolina Ciszkowicz, Ewa Lecka-Szlachta, Katarzyna Kamiński, Daniel Creaven, Bernadette Jenkins, Hollie Radomski, Piotr Miłoś, Anna Ślusarczyk, Lidia Matwijczuk, Arkadiusz Int J Mol Sci Article 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 (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) 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 MDPI 2021-09-08 /pmc/articles/PMC8471537/ /pubmed/34575894 http://dx.doi.org/10.3390/ijms22189709 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Karcz, Dariusz Starzak, Karolina Ciszkowicz, Ewa Lecka-Szlachta, Katarzyna Kamiński, Daniel Creaven, Bernadette Jenkins, Hollie Radomski, Piotr Miłoś, Anna Ślusarczyk, Lidia Matwijczuk, Arkadiusz Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors |
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 | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8471537/ https://www.ncbi.nlm.nih.gov/pubmed/34575894 http://dx.doi.org/10.3390/ijms22189709 |
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