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Rx-01_423 and Rx-01_667 are two members of the family of oxazolidinones that were designed using a combination of computational and medicinal chemistry and conventional biological techniques. The compounds have a two- to eightfold-improved potency over linezolid against serious gram-positive pathogens, including methicillin-resistantStaphylococcus aureus (MRSA), multidrug-resistant streptococci, and vancomycin-resistant enterococci. This enhanced potency extends to the coverage of linezolid-resistant gram-positive microbes, especially multidrug-resistant enterococci and pneumococci. Compounds from this series expand the spectrum compared with linezolid to include fastidious gram-negative organisms likeHaemophilus influenzae andMoraxella catarrhalis . Like linezolid, the Rx-01 compounds are bacteriostatic against MRSA and enterococci but are generally bactericidal againstS. pneumoniae andH. influenzae .

In Vitro Activities of the Rx-01 Oxazolidinones against Hospital and Community Pathogens