Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens

被引：94
|
作者：
Jarvest, RL
Berge, JM
Berry, V
Boyd, HF
Brown, MJ
Elder, JS
Forrest, AK
Fosberry, AP
Gentry, DR
Hibbs, MJ
Jaworski, DD
O'Hanlon, PJ
Pope, AJ
Rittenhouse, S
Sheppard, RJ
Slater-Radosti, C
Worby, A
机构：
[1] GlaxoSmithKline, Harlow CM19 5AW, Essex, England
[2] GlaxoSmithKline, Collegeville, PA 19426 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 10期
关键词：
D O I：
10.1021/jm025502x
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：1959 / 1962
页数：4
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