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Steroid–Au I –NHC Complexes: Synthesis and Antibacterial Activity

2017; Wiley; Volume: 12; Issue: 11 Linguagem: Inglês

10.1002/cmdc.201700257

1860-7187

Alba Vellé, Ronan Maguire, Kevin Kavanagh, Pablo J. Sanz Miguel, Diego Montagner,

Synthesis and Biological Evaluation

A series of gold(I) pioneer complexes bearing N-heterocyclic carbenes and steroid derivatives (ethynylestradiol and ethisterone) with the generic formula [Au(R2 -imidazol-2-ylidene)(steroid)] (where R=CH3 or CH2 CH2 OCH3 ) were synthesized, and the X-ray structure of a rare of gold(I)-estradiol derivative is discussed. Toxicity studies reveal notable antibacterial activity of the gold-based compounds, which is significantly increased in vivo by the presence of the estradiol unit. Toxicity profiling was estimated in vitro versus Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria, and in vivo on Galleria mellonella larvae against E. coli.