Antimicrobial Agents and Chemotherapy 2008-05-01

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

Laura Lawrence, Paul Danese, Joe DeVito, Francois Franceschi, Joyce Sutcliffe

Index: Antimicrob. Agents Chemother. 52 , 1653-62, (2008)

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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.