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

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

2021International Journal of Molecular Sciences26 citationsDOIOpen Access PDF

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

Topics & Concepts

CoumarinChemistryLigand (biochemistry)Staphylococcus epidermidisDenticityAntimicrobialMetalMetal ions in aqueous solutionAntibacterial activityAcetylcholinesteraseStereochemistryEscherichia coliNuclear chemistryStaphylococcus aureusEnzymeBacteriaBiochemistryOrganic chemistryBiologyReceptorGeneticsGeneSynthesis and biological activityMetal complexes synthesis and propertiesSynthesis and Characterization of Heterocyclic Compounds
Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors | Litcius