Aminoglycoside-Peptide Nucleic Acid (PNA) Conjugates against Gram-Negative Bacteria.

ABSTRACT: Aminoglycosides (AGs) are among the earliest known classes of antibiotics. Despite decades of clinical utility, they have become largely ineffective due to the spread of antimicrobial resistance. In an effort to improve the activity of AGs against resistant strains, we conjugated them with antisense oligonucleotides, specifically peptide nucleic acids (PNAs). We report the synthesis and biological evaluation of novel neomycin (NEO) and amikacin (AMK) conjugates with 10-mer PNA oligomers targeting the essential bacterial gene encoding the acyl carrier protein. The conjugates were prepared via copper(I)-catalyzed azide-alkyne cycloaddition between 5″-azido-modified NEO or 6″-azido-modified AMK and alkyne-functionalized PNA. The AG-PNA conjugates exhibited higher antibacterial activity agains

SUBMITTER: Siekierska I 

PROVIDER: S-EPMC12715758 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature