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Antimicrob. Agents Chemother. doi:10.1128/AAC.01383-07
Copyright (c) 2008, American Society for Microbiology and/or the Listed Authors/Institutions. All Rights Reserved.

The in vitro activity of the R -01 Oxazolidinones against Hospital and Community Pathogens

Rib-X Pharmaceuticals, Inc., 300 George Street, New Haven, Connecticut USA 06511

^* To whom correspondence should be addressed. Email: joyce.sutcliffe{at}nanobio.com.

	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 2- to 8-fold improved potency over linezolid against serious gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, 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 when 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 generally bactericidal against S. pneumoniae and H. influenzae.