Center for Silver Therapeutics Research, Department of Chemistry, The University of Akron, Akron, OH 44325-3601, USA.
Dalton Trans. 2012 Jun 7;41(21):6500-6. doi: 10.1039/c2dt00055e. Epub 2012 Mar 8.
Silver N-heterocyclic carbene complexes have been shown to have great potential as antimicrobial agents, affecting a wide spectrum of both Gram-positive and Gram-negative bacteria. A new series of three silver carbene complexes (SCCs) based on 4,5,6,7-tetrachlorobenzimidazole has been synthesized, characterized, and tested against a panel of clinical strains of bacteria. The imidazolium salts and their precursors were characterized by elemental analysis, mass spectrometry, (1)H and (13)C NMR spectroscopy, and single crystal X-ray diffraction. The silver carbene complexes, SCC32, SCC33, and SCC34 were characterized by elemental analysis, (1)H and (13)C NMR spectroscopy, and single crystal X-ray diffraction. These complexes proved highly efficacious with minimum inhibitory concentrations (MICs) ranging from 0.25 to 6 μg mL(-1). Overall, the complexes were effective against highly resistant bacteria strains, such as methicillin-resistant Staphylococcus aureus (MRSA), weaponizable bacteria, such as Yersinia pestis, and pathogens found within the lungs of cystic fibrosis patients, such as Pseudomonas aeruginosa, Alcaligenes xylosoxidans, and Burkholderia gladioli. SCC33 and SCC34 also showed clinically relevant activity against a silver-resistant strain of Escherichia coli based on MIC testing.
银氮杂环卡宾配合物已被证明具有作为抗菌剂的巨大潜力，可影响广泛的革兰氏阳性和革兰氏阴性细菌。已合成、表征了一系列基于 4,5,6,7-四氯苯并咪唑的三种银卡宾配合物（SCC），并对一组临床细菌菌株进行了测试。通过元素分析、质谱、(1)H 和 (13)C NMR 光谱以及单晶 X 射线衍射对咪唑鎓盐及其前体进行了表征。银卡宾配合物 SCC32、SCC33 和 SCC34 通过元素分析、(1)H 和 (13)C NMR 光谱以及单晶 X 射线衍射进行了表征。这些配合物的最低抑菌浓度（MIC）范围为 0.25 至 6 μg mL(-1)，证明具有高度有效性。总的来说，这些配合物对高度耐药的细菌菌株（如耐甲氧西林金黄色葡萄球菌（MRSA））、可武器化的细菌（如鼠疫耶尔森菌）以及囊性纤维化患者肺部中的病原体（如铜绿假单胞菌、木糖氧化产碱杆菌和脆弱拟杆菌）都有效。SCC33 和 SCC34 还根据 MIC 测试对一种耐银的大肠杆菌菌株显示出具有临床相关性的活性。
