title: Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.
abstract: 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.
authors: Richard L
authors: RL
authors: Jarvest
authors: John M
authors: JM
authors: Berge
authors: Valerie
authors: V
authors: Berry
authors: Helen F
authors: HF
authors: Boyd
authors: Murray J
authors: MJ
authors: Brown
authors: John S
authors: JS
authors: Elder
authors: Andrew K
authors: AK
authors: Forrest
authors: Andrew P
authors: AP
authors: Fosberry
authors: Daniel R
authors: DR
authors: Gentry
authors: Martin J
authors: MJ
authors: Hibbs
authors: Deborah D
authors: DD
authors: Jaworski
authors: Peter J
authors: PJ
authors: O'Hanlon
authors: Andrew J
authors: AJ
authors: Pope
authors: Stephen
authors: S
authors: Rittenhouse
authors: Robert J
authors: RJ
authors: Sheppard
authors: Courtney
authors: C
authors: Slater-Radosti
authors: Angela
authors: A
authors: Worby
mesh_terms: D000038:Abscess / Q000188:drug therapy / Q000382:microbiology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D024881:Drug Resistance, Bacterial; D016983:Enterococcus / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008718:Methionine-tRNA Ligase / Q000037:antagonists & inhibitors*; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013210:Staphylococcus / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D015363:Quinolones; D008718:Methionine-tRNA Ligase