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Updated: Jun 9, 2025

Synthesis of Masarimycin, a Small Molecule Inhibitor of Gram-Positive Bacterial Growth
Published on: January 7, 2022
A novel methionyl-tRNA synthetase inhibitor targeting gram-positive bacterial pathogens
Nora M R Molasky1, Zhongsheng Zhang2, J Robert Gillespie1
1Center for Emerging and Re-emerging Infectious Diseases, Department of Medicine, Division of Allergy and Infectious Disease, University of Washington, Seattle, Washington, USA.
None:
New antibiotics are needed to treat gram-positive bacterial pathogens. MRS-2541 is a novel inhibitor of methionyl-tRNA synthetase with selective activity against gram-positive bacteria. The minimum inhibitory concentrations (MICs) against Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus species range from 0.063 to 0.5 µg/mL. Given orally to mice at 50 mg/kg every 8 hours, MRS-2541 shows sustained plasma levels well above these MICs. In the mouse thigh infection model, MRS-2541 decreased methicillin-resistant Staphylococcus aureus and Streptococcus pyogenes bacterial loads to the same degree as linezolid. MRS-2541 is a promising new antibiotic for development against skin and soft tissue infections.
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