Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

新型香豆素-噻二唑杂化物及其 Cu(II) 和 Zn(II) 配合物可作为潜在的抗菌剂和乙酰胆碱酯酶抑制剂

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作者:Dariusz Karcz, Karolina Starzak, Ewa Ciszkowicz, Katarzyna Lecka-Szlachta, Daniel Kamiński, Bernadette Creaven, Hollie Jenkins, Piotr Radomski, Anna Miłoś, Lidia Ślusarczyk, Arkadiusz Matwijczuk

Abstract

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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