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Antimicrobial Agents and Chemotherapy, May 2008, p. 1653-1662, Vol. 52, No. 5
0066-4804/08/$08.00+0     doi:10.1128/AAC.01383-07
Copyright © 2008, American Society for Microbiology. All Rights Reserved.

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

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

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

Received 25 October 2007/ Returned for modification 26 November 2007/ Accepted 22 February 2008

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.

* Corresponding author. Present address: NanoBio Corporation, 2311 Green Rd., Suite A, Ann Arbor, MI 48105. Phone: (734) 302-9128. Fax: (734) 302-9150. E-mail: joyce.sutcliffe{at}nanobio.com

{triangledown} Published ahead of print on 3 March 2008.

Antimicrobial Agents and Chemotherapy, May 2008, p. 1653-1662, Vol. 52, No. 5
0066-4804/08/$08.00+0     doi:10.1128/AAC.01383-07
Copyright © 2008, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Skripkin, E., McConnell, T. S., DeVito, J., Lawrence, L., Ippolito, J. A., Duffy, E. M., Sutcliffe, J., Franceschi, F. (2008). R{chi}-01, a New Family of Oxazolidinones That Overcome Ribosome-Based Linezolid Resistance. Antimicrob. Agents Chemother. 52: 3550-3557 [Abstract] [Full Text]  


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