ABSTRACT
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.