New Broad-Spectrum Antibacterial Amphiphilic Aminoglycosides Active against Resistant Bacteria: From Neamine Derivatives to Smaller Neosamine Analogues

摘要: Aminoglycosides (AGs) constitute a major family of potent and broad-spectrum antibiotics disturbing protein synthesis through binding to the A site 16S rRNA. Decades widespread clinical use AGs strongly reduced their efficacy selection resistant bacteria. Recently, conjugation lipophilic groups generated novel class antibacterial amphiphilic aminoglycosides (AAGs) with significant improved activities against various sensitive bacterial strains. We have identified 3′,6-dialkyl derivatives small aminoglycoside neamine as broad spectrum agents targeting membranes. Here, we report on activity Gram-negative and/or Gram-positive bacteria new 3′,4′-dialkyl smaller analogues in 6-aminoglucosamine (neosamine) series prepared from N-acetylglucosamine.