Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens
Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens
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DOI：
10.1021/jm025502x
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发表时间：
2002-05-09
影响因子：
7.3
通讯作者：
Worby, A
中科院分区：
文献类型：
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作者：
Jarvest, RL;Berge, JM;Worby, A
有效的纳米摩尔金黄色葡萄球菌甲硫基tRNA合成酶抑制剂已经从一个文件化合物高通量筛选命中。优化后的化合物对葡萄球菌和肠球菌病原体（包括对临床抗生素耐药的菌株）具有良好的抗菌活性。化合物II在金黄色葡萄球菌大鼠脓肿感染模型中显示出体内有效性。
Potent nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase have been derived from a file compound high throughput screening hit. Optimized compounds show excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics. Compound II demonstrated in vivo efficacy in an S. aureus rat abscess infection model.