Zinc(II) Iminopyridine Complexes as Antibacterial Agents: A Structure-to-Activity Study

Int J Mol Sci. 2024 Apr 4;25(7):4011. doi: 10.3390/ijms25074011.

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.

Keywords: Escherichia coli; Schiff base; Staphylococcus aureus; antibiotic; bacteria; iminopyridine; metal complex; zinc.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Coordination Complexes* / pharmacology
  • Escherichia coli
  • Ligands
  • Nitrates
  • Plankton
  • Schiff Bases / pharmacology
  • Zinc* / pharmacology

Substances

  • Zinc
  • Ligands
  • Schiff Bases
  • Nitrates
  • Coordination Complexes
  • Anti-Bacterial Agents