Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366388 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
5-Deoxy-5-episubstituted arbekacin derivatives have been designed and efficiently synthesized. The synthetic compounds showed potent antibacterial activity against both Staphylococcus aureus, including methicillin-resistant S. aureus, and Pseudomonas aeruginosa. In particular, these derivatives were superior to arbekacin against MRSA strains expressing the bifunctional aminoglycoside-modifying enzyme AAC(6′)-APH(2″). The antibacterial activity of the 5-deoxy-5-episubstituted arbekacin derivatives against Pseudomonas aeruginosa was markedly influenced by the efflux system of MexXY/OprM. The 6′-N-methyl derivative of the 5-epi arbekacin was effective against Pseudomonas aeruginosa expressing the aminoglycoside-modifying enzyme AAC(6′).
Graphical abstract5-Deoxy-5-episubstituted arbekacin derivatives showed potent antibacterial activity against Staphylococcus aureus, including MRSA and Pseudomonas aeruginosa.Figure optionsDownload full-size imageDownload as PowerPoint slide