Applied Organometallic Chemistry · 2004 · 92 citations · 14 references
PharmacyChemistryMedicinal ChemistryDrug DiscoveryStructure-activity RelationshipsSynthetic Medicinal ChemistryAntibacterial PharmacologyCoordination ChemistryLigand BindingAntibacterial PropertiesAntibiotic DiscoveryBenzyl Protecting GroupsComplexation ChemistryImidazolylidene LigandsMinimum Inhibitory Concentration DeterminationNovel Antibacterial Agents
Abstract Six new 1,3‐diorganylimidazolidin‐2‐ylidene (NHC) gold(I) complexes of the type [Au(NHC) 2 ] + (1–6), were synthesized by reacting [AuCl(PPh) 3 ] with 1,3‐dimesitylimidazolidin‐2‐ylidene or bis(1,3‐dialkylimidazolidin‐2‐ylidene). The complexes 1–6 were fully characterized by elemental analyses and spectroscopic data. The placement of mesityl or para‐substituted benzyl groups on the nitrogen atoms of the ring of the complexes leads to the particularly active antibacterial agents evaluated in this work. It is worth noting that the p ‐methoxybenzyl derivative (2) inhibited the growth of Pseudomona aeruginosa, Staphylococcus epidermidis, Staphylococcus aureus and Enterococcus faecalis with minimum inhibitory concentration (MIC) values of 3.12 µg ml −1 , 6.25 µg ml −1 , 3.12 µg ml −1 and 3.12 µg ml −1 respectively. In contrast, the analogous p ‐dimethylaminobenzyl derivative (3) is effective only against Escherichia coli (MIC = 3.12 µg ml −1 ). Copyright © 2004 John Wiley & Sons, Ltd.
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