Department of Chemical Technology and Environmental Analytics (C1), Faculty of Chemical Engineering and Technology, Cracow University of Technology, 31-155 Kraków, Poland.
Department of Biotechnology and Bioinformatics, Faculty of Chemistry, Rzeszow University of Technology, 35-959 Rzeszów, Poland.
Int J Mol Sci. 2021 Sep 8;22(18):9709. doi: 10.3390/ijms22189709.
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 (, ) and Gram-negative (, ) 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.
一系列香豆素-噻二唑杂化物及其相应的 Cu(II) 和 Zn(II) 配合物被合成并通过光谱技术进行了表征。结果表明，所有香豆素-噻二唑杂化物均作为 Cu(II) 和 Zn(II) 离子的双齿螯合剂。分离出的配合物的配体：金属比取决于中心金属而有所不同。在大多数情况下，Zn(II) 配合物的配体：金属比为 1:1，而在 Cu(II) 配合物中，配体：金属比为 2:1。所有化合物均被测试为潜在的抗菌剂，对抗革兰氏阳性（ ， ）和革兰氏阴性（ ， ）细菌菌株，其活性明显低于市售抗生素。从评估神经退行性疾病潜力方面获得了更有希望的结果，因为所有化合物均显示出适度的乙酰胆碱酯酶（AChE）抑制活性。
