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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...

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Autores principales: Karcz, Dariusz, Starzak, Karolina, Ciszkowicz, Ewa, Lecka-Szlachta, Katarzyna, Kamiński, Daniel, Creaven, Bernadette, Jenkins, Hollie, Radomski, Piotr, Miłoś, Anna, Ślusarczyk, Lidia, Matwijczuk, Arkadiusz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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
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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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