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Updated: Aug 30, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Novel oxazolidinone-quinolone hybrid antimicrobials
Mikhail F Gordeev1, Corinne Hackbarth, Michael R Barbachyn
1Vicuron Pharmaceuticals Inc., 34790 Ardentech Ct., Fremont, CA 94555, USA. mgordeev@vicuron.com
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.
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