新型抗耐甲氧西林金黄色葡萄球菌和抗耐万古霉素肠球菌药物——双阳离子双苯并咪唑类化合物的合成及其体外活性
Synthesis and in vitro activity of dicationic bis-benzimidazoles as a new class of anti-MRSA and anti-VRE agents.
作者信息
Hu Laixing, Kully Maureen L, Boykin David W, Abood Norman
机构信息
Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1292-5. doi: 10.1016/j.bmcl.2009.01.075. Epub 2009 Feb 7.
A new class of novel bis-benzimidazole diamidine compounds have been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Anti-MRSA and anti-VRE activities of the most potent compound 1 were more active than Vancomycin. The mechanism of action for this class of compounds appears to be different from existing antibiotics. Bis-benzimidazole diamidine compounds have potential for further investigation as a new class of potent anti-MRSA and anti-VRE agents.
一类新型的双苯并咪唑二脒化合物已被合成并评估其体外抗菌活性，包括对耐药菌株的活性。最有效的化合物1的抗耐甲氧西林金黄色葡萄球菌（MRSA）和抗耐万古霉素肠球菌（VRE）活性比万古霉素更强。这类化合物的作用机制似乎与现有抗生素不同。双苯并咪唑二脒化合物有潜力作为一类新型强效抗MRSA和抗VRE药物进行进一步研究。
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