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

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 (C2B10H12, carboranes). The hetero‐ and homoleptic merca...

Full description

Saved in:
Bibliographic Details
Published inChemPlusChem (Weinheim, Germany) Vol. 89; no. 6; pp. e202300759 - n/a
Main Authors Selg, Christoph, Grell, Toni, Brakel, Alexandra, Andrews, Philip C., Hoffmann, Ralf, Hey‐Hawkins, Evamarie
Format Journal Article
LanguageEnglish
Published Germany 01.06.2024
Subjects
antibiotics
antimicrobial compound
bismuth
carborane
mercaptocarborane
mercaptocarborane
antimicrobial compound
carborane
antibiotics
bismuth
Online AccessGet full text

Cover

More Information
Summary: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 (C2B10H12, carboranes). The hetero‐ and homoleptic mercaptocarborane complexes BiPh2L (1) and BiL3 (2) (L=9‐S‐1,2‐C2B10H11) 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. An ace up the sleeves: A novel approach to refine the pharmacophore model for antimicrobial bismuth thiolato complexes is introduced. By substitution of conventional ligands with carboranes, hetero‐ and homoleptic carboranylthiolato complexes were synthesised and biologically evaluated. Effective against the Gram‐positive S. aureus with single‐digit μm minimum inhibitory concentrations, they present a compelling avenue for antimicrobial research.
Bibliography:The authors contributed equally to the manuscript.
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:2192-6506
2192-6506
DOI:10.1002/cplu.202300759