Novel oxazolidinone–quinolone hybrid antimicrobials
| Autor: | Gary W. Luehr, Jonathan M. Evans, Gage James R, Barbachyn Michael R, Joaquim Trias, Christian N. Parker, Lee S. Banitt, Gary E. Zurenko, Sara E. Morin, Dinesh V. Patel, Mikhail F. Gordeev, C. Hackbarth, Richard White, Marcela Gomez |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
DNA Topoisomerase IV
medicine.drug_class Stereochemistry Topoisomerase IV Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Quinolones Gram-Positive Bacteria Biochemistry DNA gyrase Microbiology Structure-Activity Relationship chemistry.chemical_compound Ciprofloxacin Acetamides Drug Resistance Bacterial Gram-Negative Bacteria Drug Discovery medicine Molecular Biology Oxazolidinones Antibacterial agent Molecular Structure biology Chemistry Organic Chemistry Linezolid biochemical phenomena metabolism and nutrition Quinolone biology.organism_classification Antimicrobial Anti-Bacterial Agents biology.protein Molecular Medicine Pharmacophore Enterococcus faecium |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:4213-4216 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2003.07.021 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect