Solution studies, synthesis and antibacterial activity of Ga(III) complexes with bis-kojate derivatives

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

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Article number112663
JournalJournal of Inorganic Biochemistry
Volume259
DOIs
Publication statusPublished - Oct 2024

Keywords

  • Antibacterial
  • Bis-kojic acid
  • Gallium
  • Hydroxypyrones
  • Metallophores
  • P. aeruginosa

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