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ID: ALA1255340

Journal: Antimicrob Agents Chemother

Title: In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.

Authors: Lawrence L, Danese P, DeVito J, Franceschi F, Sutcliffe J.

Abstract: 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-resistant Staphylococcus 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 like Haemophilus influenzae and Moraxella catarrhalis. Like linezolid, the Rx-01 compounds are bacteriostatic against MRSA and enterococci but are generally bactericidal against S. pneumoniae and H. influenzae.

CiteXplore: 18316525

DOI: 10.1128/aac.01383-07