Discovery of an Octahedral Silicon Complex as a Potent Antifungal Agent

Molecules. 2017 Apr 15;22(4):637. doi: 10.3390/molecules22040637.

Abstract

Octahedral transition metal complexes have been shown to have tremendous applications in chemical biology and medicinal chemistry. Meanwhile, structural transition metals can be replaced by inert octahedral silicon in a proof-of-principle study. We here introduce the first example of octahedral silicon complexes, which can very well serve as an efficient antimicrobial agent. The typical silicon arenediolate complex 1 {[(phen)₂Si(OO)](PF₆)₂, with phen = 1,10-phenanthroline, OO = 9,10-phenanthrenediolate} exhibited significant inhibition towards the growth of Cryptococcus neoformans with MIC and MFC values of 4.5 and 11.3 μM, respectively. Moreover, it was fungicidal against both proliferative and quiescent Cryptococcus cells. This work may set the stage for the development of novel antifungal drugs based upon hexacoodinate silicon scaffolds.

Keywords: antifungal agent; antimicrobial activity; octahedral complex; silicon.

MeSH terms

  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology*
  • Aza Compounds / chemistry*
  • Bridged-Ring Compounds / chemistry*
  • Cryptococcus neoformans / drug effects
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Molecular Structure
  • Silicon / chemistry*

Substances

  • Antifungal Agents
  • Aza Compounds
  • Bridged-Ring Compounds
  • octahedrane
  • Silicon