Open AccessIn Vitro Activities of the Rx-01 Oxazolidinones against Hospital and Community Pathogens
Author(s) -
Laura Lawrence,
Paul N. Danese,
J. A. DeVito,
F. Franceschi,
Joyce A. Sutcliffe
Publication year - 2008
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.01383-07
Subject(s) - linezolid , moraxella catarrhalis , fastidious organism , microbiology and biotechnology , haemophilus influenzae , staphylococcus aureus , potency , moraxella , streptococcus pneumoniae , methicillin resistant staphylococcus aureus , antibiotics , enterococcus , multiple drug resistance , vancomycin , biology , medicine , in vitro , bacteria , biochemistry , genetics
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 .
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