Laboratory of Organic Chemistry, School of Chemical Engineering, National Technical University of Athens, Zografou Campus, Athens, Greece.
Institute of Biosciences and Applications, National Center for Scientific Research "Demokritos", Ag. Paraskevi, Attiki, Greece.
Arch Pharm (Weinheim). 2021 Dec;354(12):e2100305. doi: 10.1002/ardp.202100305. Epub 2021 Sep 27.
The synthesis and biological evaluation of 5-arylidene-N-acetyl-tetramic acids cadmium(II) complexes are reported. Eleven novel compounds were prepared, characterized by nuclear magnetic resonance experiments and screened for their antimicrobial activity against five bacterial species (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and methicillin-resistant Staphylococcus aureus [MRSA]) and two fungi (Candida albicans and Cryptococcus neoformans). The complexes showed similar or enhanced activities against MRSA in comparison to the corresponding ligands and, additionally, promising antifungal activities against C. neoformans. The most active compounds 3c and 3h showed remarkable activities against MRSA (minimum inhibitory activity [MIC] values of 32 and 4 μg/ml, respectively) and C. neoformans (MIC values of 8 and 16 μg/ml, respectively), accompanied by no human cell toxicity and hemolytic activity within the tested concentration range. The results demonstrate that appropriately functionalized tetramic acids attached with lipophilic alkanoyl chain and after complexation with cadmium(II) ions may act as valuable lead compounds for further investigations toward the development of novel antibacterial and/or antifungal agents.
报告了 5-芳亚甲基-N-乙酰四氢酸镉（II）配合物的合成和生物评价。合成了 11 种新型化合物，通过核磁共振实验对其进行了表征，并对它们的抗菌活性进行了筛选，以评估它们对五种细菌（大肠杆菌、肺炎克雷伯菌、鲍曼不动杆菌、铜绿假单胞菌和耐甲氧西林金黄色葡萄球菌[MRSA]）和两种真菌（白色念珠菌和新型隐球菌）的抑制作用。与相应的配体相比，这些配合物对 MRSA 的活性相似或增强，并且对新型隐球菌具有有前景的抗真菌活性。最有效的化合物 3c 和 3h 对 MRSA（最小抑菌浓度 [MIC] 值分别为 32 和 4 μg/ml）和新型隐球菌（MIC 值分别为 8 和 16 μg/ml）表现出显著的活性，并且在测试浓度范围内对人细胞没有毒性和溶血活性。结果表明，适当功能化的与脂酰链相连的四氢酸，与镉（II）离子配位后，可能成为进一步研究开发新型抗菌和/或抗真菌药物的有价值的先导化合物。
