Abstract The limited scope of antiviral drugs and increasing problem of antiviral drug resistance represent a global health threat. Glycopeptide antibiotics and their lipophilic derivatives have emerged as relevant inhibitors of diverse viruses. Herein, we describe a new strategy for the synthesis of dual hydrophobic and lipophobic derivatives of glycopeptides to produce selective antiviral agents without membrane‐disrupting activity. Perfluorobutyl and perfluorooctyl moieties were attached through linkers of different length to azido derivatives of vancomycin aglycone and teicoplanin pseudoaglycone, and the new derivatives were evaluated against a diverse panel of viruses. The teicoplanin derivatives displayed strong anti‐influenza virus activity at nontoxic concentrations. Some of the perfluoroalkylated glycopeptides were also active against a few other viruses such as herpes simplex virus or coronavirus. These data encourage further exploration of glycopeptide analogues for broad antiviral application. Plan F : Perfluoroalkylated blocks were incorporated into azido glycopeptide derivatives of vancomycin and teicoplanin. The teicoplanin derivatives displayed strong antiviral activity against a diverse panel of viruses at nontoxic concentrations. The vancomycin derivatives showed cytotoxicity, while being inactive against influenza viruses. Perfluorobutylated teicoplanins displayed excellent antibacterial activity against a panel of Gram‐positive bacteria.
【저자키워드】 coronavirus, Antiviral, Influenza virus, glycopeptide antibiotic, perfluoroalkyl, 【초록키워드】 viruses, cytotoxicity, Antibiotics, antiviral activity, virus, antiviral drug, Health, influenza viruses, Bacteria, antiviral agent, inhibitor, hydrophobic, plan, selective, derivative, herpes simplex, analogue, block, concentrations, linker, evaluated, active against, inactive, nontoxic, 【제목키워드】 synthesis, Teicoplanin, derivative, vancomycin,