Jarvest Richard L, Berge John M, Berry Valerie, Boyd Helen F, Brown Murray J, Elder John S, Forrest Andrew K, Fosberry Andrew P, Gentry Daniel R, Hibbs Martin J, Jaworski Deborah D, O'Hanlon Peter J, Pope Andrew J, Rittenhouse Stephen, Sheppard Robert J, Slater-Radosti Courtney, Worby Angela
J Med Chem. 2002 May 9;45(10):1959-62. doi: 10.1021/jm025502x.
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 11 demonstrated in vivo efficacy in an S. aureus rat abscess infection model.
金黄色葡萄球菌甲硫氨酰-tRNA合成酶的强效纳摩尔抑制剂已从一个存档化合物高通量筛选命中物中获得。优化后的化合物对葡萄球菌和肠球菌病原体表现出优异的抗菌活性，包括对临床抗生素耐药的菌株。化合物11在金黄色葡萄球菌大鼠脓肿感染模型中显示出体内疗效。
