双蒟蒻酸盐衍生物的 Ga(III) 复合物的溶液研究、合成和抗菌活性

IF 3.8 2区 化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Journal of Inorganic Biochemistry Pub Date : 2024-07-14 DOI:10.1016/j.jinorgbio.2024.112663
L. More O'Ferrall , A. Fantasia , K. Chan , L.M. Teixeira , K. Kavanagh , C. O'Connor , M.A. Santos , S. Chaves , V.M. Nurchi , G. Crisponi , M.A. Zoroddu , D.M. Griffith , R. Cappai
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引用次数: 0

摘要

鉴于微生物的耐药性是人类健康公认的重大问题,目前人们一直在探索新的金属基药物的抗菌特性,其中包括作为潜在金属载体的镓基化合物,它们可以扰乱铁与蛋白质的相互作用。在此,我们设计并合成了两种双kojate 配体(分别命名为 L4 和 L6),并研究了它们的 Ga(III) 复合物的物理化学和生物学特性。特别是对它们在水溶液中的络合性质进行的详细研究表明,它们形成了相当稳定的双核 2:3 金属:配体络合物的平衡模型,尽管它们的稳定性各不相同。固态配合物的制备和表征以及 DFT 补充研究表明,[Ga2(L4)3] 配合物具有更高的稳定性,似乎采用了三配体桥接构象,而 L6 采用了单配体桥接构象。对这些镓配合物抗菌活性的初步研究表明,L4 配合物具有较高的抗伪菌活性,这一特性可能会引起科学界的兴趣。
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Solution studies, synthesis and antibacterial activity of Ga(III) complexes with bis-kojate derivatives

Given the recognized major problem of microbial drug resistance for human health, new metal-based drugs have been currently explored for their antimicrobial properties, including gallium-based compounds as potential metallophores that could perturb Fe’s interactions with proteins. Herein we have designed and synthesized two bis-kojate ligands (named L4 and L6) and studied their Ga(III) complexes for their physico-chemical and biological properties. In particular a detailed study of their complexation properties in aqueous solution, showed equilibrium models with formation of quite stable dinuclear 2:3 metal:ligand complexes, though with different stability. Solid state complexes were also prepared and characterized and complementary DFT studies indicated that [Ga2(L4)3] complex, with higher stability, seems to adopt a three-ligand bridging conformation, while that for L6 adopt a one ligand bridging conformation. Preliminary investigation of the antibacterial activity of these gallium complexes showed antipseudomonal activity, which appeared higher for the complex with L4, a feature of potential interest for the scientific community.

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来源期刊
Journal of Inorganic Biochemistry
Journal of Inorganic Biochemistry 生物-生化与分子生物学
CiteScore
7.00
自引率
10.30%
发文量
336
审稿时长
41 days
期刊介绍: The Journal of Inorganic Biochemistry is an established international forum for research in all aspects of Biological Inorganic Chemistry. Original papers of a high scientific level are published in the form of Articles (full length papers), Short Communications, Focused Reviews and Bioinorganic Methods. Topics include: the chemistry, structure and function of metalloenzymes; the interaction of inorganic ions and molecules with proteins and nucleic acids; the synthesis and properties of coordination complexes of biological interest including both structural and functional model systems; the function of metal- containing systems in the regulation of gene expression; the role of metals in medicine; the application of spectroscopic methods to determine the structure of metallobiomolecules; the preparation and characterization of metal-based biomaterials; and related systems. The emphasis of the Journal is on the structure and mechanism of action of metallobiomolecules.
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