Author/Authors :
Mikhail F. Gordeev، نويسنده , , Corinne Hackbarth، نويسنده , , Michael R. Barbachyn، نويسنده , , Lee S. Banitt، نويسنده , , James R. Gage، نويسنده , , Gary W. Luehr، نويسنده , , Marcela Gomez، نويسنده , , Joaquim Trias، نويسنده , , Sara E. Morin، نويسنده , , Gary E. Zurenko، نويسنده , , Christian N. Parker، نويسنده , , Jonathan M. Evans، نويسنده , , Richard J. White، نويسنده , , Dinesh V. Patel، نويسنده ,
Abstract :
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.
