Molasky Nora M R, Zhang Zhongsheng, Gillespie J Robert, Domagala John, Reyna Dawn, Lipka Elke, Fan Erkang, Buckner Frederick S
Center for Emerging and Re-emerging Infectious Diseases, Department of Medicine, Division of Allergy and Infectious Disease, University of Washington, Seattle, Washington, USA.
Department of Biochemistry, University of Washington, Seattle, Washington, USA.
Antimicrob Agents Chemother. 2024 Dec 5;68(12):e0074524. doi: 10.1128/aac.00745-24. Epub 2024 Oct 29.
New antibiotics are needed to treat gram-positive bacterial pathogens. is a novel inhibitor of methionyl-tRNA synthetase with selective activity against gram-positive bacteria. The minimum inhibitory concentrations (MICs) against and species range from 0.063 to 0.5 µg/mL. Given orally to mice at 50 mg/kg every 8 hours, shows sustained plasma levels well above these MICs. In the mouse thigh infection model, decreased methicillin-resistant and bacterial loads to the same degree as linezolid. is a promising new antibiotic for development against skin and soft tissue infections.
需要新型抗生素来治疗革兰氏阳性菌病原体。[药物名称]是一种新型甲硫氨酰 - tRNA合成酶抑制剂，对革兰氏阳性菌具有选择性活性。对[具体细菌名称1]和[具体细菌名称2]菌种的最低抑菌浓度（MIC）范围为0.063至0.5μg/mL。以50mg/kg的剂量每8小时给小鼠口服[药物名称]，其血浆水平持续维持在远高于这些MIC的水平。在小鼠大腿感染模型中，[药物名称]将耐甲氧西林的[具体细菌名称1]和[具体细菌名称2]细菌载量降低到与利奈唑胺相同的程度。[药物名称]是一种有前景的新型抗生素，可用于开发治疗皮肤和软组织感染。
