C07D285/00

Simplified structural mimetics of AIPS as quorum sensing inhibitors

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I: ##STR00001##
or salts or solvates thereof, where variables R, W, X.sub.1, X.sub.2, and Z and are as described in the specification and L.sub.1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds 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 that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I: ##STR00001##
or salts or solvates thereof, where variables R, W, X.sub.1, X.sub.2, and Z and are as described in the specification and L.sub.1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds 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
20230094587 · 2023-03-30 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I:

##STR00001##

or salts or solvates thereof, where variables R, W, X.sub.1, X.sub.2, and Z and are as described in the specification and L.sub.1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds 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
20230094587 · 2023-03-30 ·

Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds provided are racemic, non-racemic or substantially enantiomerically pure cyclic peptides of formula I:

##STR00001##

or salts or solvates thereof, where variables R, W, X.sub.1, X.sub.2, and Z and are as described in the specification and L.sub.1 is a divalent linker which contains 1-12 carbon atoms, optionally 1-4 oxygen atoms, optionally one or two carbon-carbon double bonds, and hydrogen atoms to satisfy valency. Certain dimers of the cyclic peptides are also provided. One or more cylic peptides or dimers thereof herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.

Modulators of Alpha-4-beta-7 Integrin and MAdCAM
20230145835 · 2023-05-11 ·

The instant disclosure describes novel modulators of alpha α4β7 and/or MAdCAM and their use for the treatment of diseases and conditions associated with their biological function. Further described herein are methods of treating diseases or conditions associated with α4β7 and/or MAdCAM.

Modulators of Alpha-4-beta-7 Integrin and MAdCAM
20230145835 · 2023-05-11 ·

The instant disclosure describes novel modulators of alpha α4β7 and/or MAdCAM and their use for the treatment of diseases and conditions associated with their biological function. Further described herein are methods of treating diseases or conditions associated with α4β7 and/or MAdCAM.

Synthesis of syrbactin proteasome inhibitors

The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs.

Synthesis of syrbactin proteasome inhibitors

The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs.

Methods and compositions for diagnosis and management of neurodegerative diseases

Described herein are assays, methods, and devices for diagnosing/prognosing Alzheimer's disease (AD) and/or a neurodegenerative disease in a subject. The assays, methods, and/or devices described herein can be configured to detect GAS5 long-coding RNAs and/or expression thereof in a sample from a subject.