PDF(Pubmed)
Abstract：
Antibiotic resistance is currently a global health emergency. Metallodrugs, especially metal coordination complexes, comprise a broad variety of candidates to combat antibacterial infections. In this work, we designed a new family of Schiff base zinc(II) complexes with iminopyridine as an organic ligand and different inorganic ligands: chloride, nitrate, and acetate. The antibacterial effect of the Zn(II) complexes was studied against planktonic bacterial cells of Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) strains. The results showed a moderate biocide activity in both types of planktonic bacteria, which arises from the metal complexation to the Schiff base ligand. Importantly, we confirmed the crucial effect of the metal, with Zn(II) improving the activity of Cu(II) counterparts previously reported. On the other hand, the impact of the inorganic ligands was not significant for the antibacterial effect but was relevant for the complex solubility. Finally, as proof of concept of topical antibacterial formulation, we formulated an emulsion containing the most lipophilic Zn(II) complex and confirmed a sustained release for 24 h in a vertical cell diffusion assay. The promising activity of iminopyridine Zn(II) complexes is potentially worth exploring in more detailed studies.
摘要：
抗生素耐药性目前是全球卫生紧急情况。金属药物,特别是金属配位络合物，包括各种各样的候选人，以对抗抗菌感染。在这项工作中,我们设计了一个新的席夫碱锌（II）配合物家族，以亚氨基吡啶作为有机配体和不同的无机配体：氯化物，硝酸盐,和醋酸盐。研究了Zn（II）复合物对金黄色葡萄球菌（革兰氏阳性）和大肠杆菌（革兰氏阴性）菌株的浮游细菌细胞的抗菌作用。结果表明，在这两种类型的浮游细菌中具有中等的杀生物活性，这是由金属与席夫碱配体的络合引起的。重要的是,我们证实了金属的重要作用，Zn（II）提高了以前报道的Cu（II）对应物的活性。另一方面,无机配体对抗菌作用的影响不明显，但与配合物的溶解度有关。最后,作为局部抗菌制剂概念的证明，我们配制了含有最亲脂性锌（II）复合物的乳剂，并在垂直细胞扩散测定法中证实了24小时的持续释放。亚氨基吡啶Zn（II）配合物的有希望的活性可能值得在更详细的研究中探索。
