C07D291/02

Simplified Structural Mimetics of AIPS as Quorum Sensing Inhibitors
20180170889 · 2018-06-21 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.

Simplified Structural Mimetics of AIPS as Quorum Sensing Inhibitors
20180170889 · 2018-06-21 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.

Simplified structural mimetics of AIPS as quorum sensing inhibitors

Compounds provided are racemic, non-racemic or substantially enantiomerically pure dimers or salts or solvates thereof of formula: ##STR00001## where: W and W are S or NR.sub.1, or WCO or WCO is CHCH, where each R.sub.1 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R and R are hydrogen or an straight-chain or branched alkyl group having 1-3 carbon atoms; R.sub.3 and R.sub.3 are hydrogen or a C1-C3 alkyl; X.sub.1, X.sub.1, X.sub.2 and X.sub.2 are optionally-substituted straight-chain or branched alkyl groups having 3-8 carbon atoms, optionally-substituted cycloalkyl groups having 3-12 carbon atoms; optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted heterocycyl, optionally-substituted cycloalkylalkyl, optionally-substituted arylalkyl, optionally-substituted heteroarylalkyl and optionally-substituted heterocycylalkyl groups and L.sub.1, L.sub.1 and L.sub.2 are divalent chemical moieties. Dimers are employed to modulate quorum sensing and to thus inhibit virulence in Staphylococcus bacteria. Dimers are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.

Simplified structural mimetics of AIPS as quorum sensing inhibitors

Compounds provided are racemic, non-racemic or substantially enantiomerically pure dimers or salts or solvates thereof of formula: ##STR00001## where: W and W are S or NR.sub.1, or WCO or WCO is CHCH, where each R.sub.1 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R and R are hydrogen or an straight-chain or branched alkyl group having 1-3 carbon atoms; R.sub.3 and R.sub.3 are hydrogen or a C1-C3 alkyl; X.sub.1, X.sub.1, X.sub.2 and X.sub.2 are optionally-substituted straight-chain or branched alkyl groups having 3-8 carbon atoms, optionally-substituted cycloalkyl groups having 3-12 carbon atoms; optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted heterocycyl, optionally-substituted cycloalkylalkyl, optionally-substituted arylalkyl, optionally-substituted heteroarylalkyl and optionally-substituted heterocycylalkyl groups and L.sub.1, L.sub.1 and L.sub.2 are divalent chemical moieties. Dimers are employed to modulate quorum sensing and to thus inhibit virulence in Staphylococcus bacteria. Dimers are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease