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Fusing Bismuth and Mercaptocarboranes: Design and Biological Evaluation of Low-Toxicity Antimicrobial Thiolato Complexes.

Christoph SelgToni GrellAlexandra BrakelPhilip C AndrewsRalf HoffmannEvamarie Hey-Hawkins
Published in: ChemPlusChem (2024)
This study proposes an innovative strategy to enhance the pharmacophore model of antimicrobial bismuth thiolato complex drugs by substituting hydrocarbon ligand structures with boron clusters, particularly icosahedral closo-dicarbadodecaborane (C 2 B 10 H 12 , carboranes). The hetero- and homoleptic mercaptocarborane complexes BiPh 2 L (1) and BiL 3 (2) (L=9-S-1,2-C 2 B 10 H 11 ) were prepared from 9-mercaptocarborane (HL) and triphenylbismuth. Comprehensive characterization using NMR, IR, MS, and XRD techniques confirmed their successful synthesis. Evaluation of antimicrobial activity in a liquid broth microdilution assay demonstrated micromolar to submicromolar minimum inhibitory concentrations (MIC) suggesting high effectiveness against S. aureus and limited efficacy against E. coli. This study highlights the potential of boron-containing bismuth complexes as promising antimicrobial agents, especially targeting Gram-positive bacteria, thus contributing to the advancement of novel therapeutic approaches.
Keyphrases
  • staphylococcus aureus
  • randomized controlled trial
  • magnetic resonance
  • escherichia coli
  • mass spectrometry
  • ms ms
  • risk assessment
  • gram negative
  • ionic liquid
  • molecular dynamics
  • molecular docking
  • human health