A series of polymeric silver(I) complexes with Schiff base ligands containing pyridine and 3,5‐halogen substituted phenol moieties were synthesized and characterized by spectroscopic methods and in the case of Ag6 also by X‐ray crystallography. All silver(I) complexes (Ag1–Ag8) were evaluated for their biological activity against a panel of pathogens including the protozoa Trypanosoma cruzi, T. brucei, T. rhodesiense and Leishmania infantum; the bacteria Staphylococcus aureus, Escherichia coli, Mycobacterium tuberculosis H37Ra and the yeast Candida albicans. Cytotoxicity evaluation was carried out on human lung fibroblasts (MRC‐5) and on primary peritoneal mouse macrophages. The most relevant result reveals antileishmanial activity potential with all complexes demonstrating higher potency than the reference drug miltefosine. Complexes with the best antiprotozoal profile (i.e., Ag2 and Ag7) were selected for incorporation into poly (lactic acid) nanoparticles (PLA NPs) with the aim to enhance selectivity. PLA/Ag2 NPs and PLA/Ag7 NPs exhibited adequate physicochemical properties, that is, average size of 263 ± 60 nm and 225 ± 6 nm, respectively, good entrapment efficiency (69% and 63%), loading content (6.2% and 5.7%) and stability. The cytotoxicity of PLA/Ag2 NPs and PLA/Ag7 NPs on MRC‐5 cells was reduced with respect to the “free” metal complexes by ~2‐fold and ~6‐fold, respectively.

中文翻译：

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源自不对称卤代席夫碱配体的银配位聚合物的抗菌和抗原虫活性

合成了一系列具有席夫碱配体的聚合银（I）配合物，该席夫碱配体包含吡啶和3,5-卤素取代的酚部分，并通过分光镜方法进行了表征，对于Ag6，还通过X射线晶体学对其进行了表征。所有银（I）配合物（Ag1-Ag8）对一组病原体的生物学活性进行了评估，包括原生动物克氏锥虫，布氏锥虫，罗德氏梭菌和利什曼原虫; 细菌金黄色葡萄球菌，大肠杆菌，结核分枝杆菌H37Ra的和酵母白色念珠菌。对人肺成纤维细胞（MRC-5）和原代腹膜小鼠巨噬细胞进行了细胞毒性评估。最相关的结果表明，所有复合物的抗衰老活性均高于参比药物米替福辛。选择具有最佳抗原生动物谱的复合物（即Ag2和Ag7）以掺入聚（乳酸）纳米颗粒（PLA NPs）中，以提高选择性。PLA / Ag2 NP和PLA / Ag7 NP表现出足够的理化特性，即平均大小分别为263±60 nm和225±6 nm，良好的包封率（69％和63％），负载量（6.2％和5.7） ％）和稳定性。PLA / Ag2 NPs和PLA / Ag7 NPs对MRC-5细胞的细胞毒性相对于“游离”金属配合物分别降低了约2倍和约6倍。