444335-14-2Relevant articles and documents
Novel oxazolidinone-quinolone hybrid antimicrobials
Gordeev, Mikhail F.,Hackbarth, Corinne,Barbachyn, Michael R.,Banitt, Lee S.,Gage, James R.,Luehr, Gary W.,Gomez, Marcela,Trias, Joaquim,Morin, Sara E.,Zurenko, Gary E.,Parker, Christian N.,Evans, Jonathan M.,White, Richard J.,Patel, Dinesh V.
, p. 4213 - 4216 (2007/10/03)
Antimicrobial compounds incorporating oxazolidinone and quinolone pharmacophore substructures have been synthesized and evaluated. Representative analogues 2, 5, and 6 display an improved potency versus linezolid against gram-positive and fastidious gram-negative pathogens. The compounds are also active against linezolid- and ciprofloxacin-resistant Staphylococcus aureus and Enterococcus faecium strains. The MOA for these new antimicrobials is consistent with a combination of protein synthesis and gyrase A/topoisomerase IV inhibition, with a structure-dependent degree of the contribution from each inhibitory mechanism.