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.

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.

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I):

##STR00001##

including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.

The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q.sub.1, Q.sub.2, Q.sub.3, R.sub.8 and R.sub.9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The application relates to fluorescence-quenched substrates of Formula (I) for an acid -glucosidase (GCase) and their use in a method for determining GCase activity in a cell or tissue, a method for localizing GCase activity within a cell, a method for determining the effect of a GCase modulator in a cell, a method for determining the efficacy if a GCase-directed therapy, and a method of screening for a GCase activity enhancer.

##STR00001##

The application relates to fluorescence-quenched substrates of Formula (I) for an acid -glucosidase (GCase) and their use in a method for determining GCase activity in a cell or tissue, a method for localizing GCase activity within a cell, a method for determining the effect of a GCase modulator in a cell, a method for determining the efficacy if a GCase-directed therapy, and a method of screening for a GCase activity enhancer.

##STR00001##