Jarvest Richard L, Berge John M, Brown Murray J, Brown Pamela, Elder John S, Forrest Andrew K, Houge-Frydrych C S V, O'Hanlon Peter J, McNair David J, Rittenhouse Stephen, Sheppard Robert J
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Bioorg Med Chem Lett. 2003 Feb 24;13(4):665-8. doi: 10.1016/s0960-894x(02)01027-2.
Optimisation of the left-hand-side aryl moiety of a file compound screening hit against Staphylococcus aureus methionyl tRNA synthetase led to the identification of a series of potent nanomolar inhibitors. The best compounds showed excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics.
针对金黄色葡萄球菌甲硫氨酰 - tRNA合成酶对先导化合物筛选命中物的左侧芳基部分进行优化，从而鉴定出一系列强效的纳摩尔级抑制剂。最佳化合物对葡萄球菌和肠球菌病原体显示出优异的抗菌活性，包括对临床抗生素耐药的菌株。
