Design, Synthesis, and Biological Evaluation of 6″-Modified Apramycin Derivatives to Overcome Aminoglycoside Resistance.

ABSTRACT: Background/Objectives: Despite their long history of clinical use, aminoglycosides remain important broad-spectrum antibiotics, exhibiting potent activity against Gram-positive, Gram-negative, and mycobacterial pathogens. However, the growing prevalence of antimicrobial resistance, along with the well-documented nephrotoxicity and ototoxicity associated with this class, underscores the urgent need for novel derivatives with enhanced pharmacological and safety profiles. Methods: In this study, we developed a synthetic approach for the synthesis of new apramycin derivatives featuring structural modifications at the 6″-position of 4-amino-4-deoxy-D-glucose residue, specifically through the introduction of aminoalkylamine and guanidinoalkylamine substituents. The synthesized comp

SUBMITTER: Shapovalova KS 

PROVIDER: S-EPMC12736951 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature