Abstract: The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.

Abstract: The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6?, C2? and/or C5?. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

Abstract: The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6?, C2? and/or C5?. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

Abstract: The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.

Abstract: The present invention is directed to a method for identifying ribosomal antimicrobial substances being selective for microbial but not for mitochondrial and/or cytosolic ribosomes. Specifically, said method is directed to an assay that compares the interaction of a candidate ribosomal antimicrobial substance (i) in a bacterial strain with microbial ribosomes, and (ii) in a bacterial strain with chimeric mitochondrial bacterial ribosomes, and/or (iii) in a bacterial strain with chimeric cytosolic bacterial ribosomes. In a further aspect the present invention also relates to the use of bacterial strains with microbial ribosomes, and bacterial strains with chimeric mitochondrial bacterial ribosomes, and/or bacterial strains with chimeric cytosolic bacterial ribosomes for identifying ribosomal antimicrobial substance being selective for microbial but not for mitochondrial and/or cytosolic ribosomes.

Abstract: The present invention is directed to a method for identifying ribosomal antimicrobial substances being selective for microbial but not for mitochondrial and/or cytosolic ribosomes. Specifically, said method is directed to an assay that compares the interaction of a candidate ribosomal antimicrobial substance (i) in a bacterial strain with microbial ribosomes, and (ii) in a bacterial strain with chimeric mitochondrial bacterial ribosomes, and/or (iii) in a bacterial strain with chimeric cytosolic bacterial ribosomes. In a further aspect the present invention also relates to the use of bacterial strains with microbial ribosomes, and bacterial strains with chimeric mitochondrial bacterial ribosomes, and/or bacterial strains with chimeric cytosolic bacterial ribosomes for identifying ribosomal antimicrobial substance being selective for microbial but not for mitochondrial and/or cytosolic ribosomes.