In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
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.
Lawrence
Laura
L
Rib-X Pharmaceuticals, Inc., 300 George Street, New Haven, Connecticut 06511, USA.
Danese
Paul
P
DeVito
Joe
J
Franceschi
Francois
F
Sutcliffe
Joyce
J
D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D017714:Community-Acquired Infections / Q000382:microbiology; D003428:Cross Infection / Q000382:microbiology; D016983:Enterococcus / Q000187:drug effects; D006801:Humans; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology*; D012137:Respiratory System / Q000382:microbiology; D013210:Staphylococcus / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects
D000890:Anti-Infective Agents; D023303:Oxazolidinones