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.

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.

The present disclosure provides macrocyclic compounds comprising a 4-amido-2,4-pentadienoate (APD) moiety. The compounds exhibit toxicity that is selective to the hypoxic micro-environments often found in cancerous tissues. The disclosed compounds are therefore suitable for treatment of hypoxic cancer cells.

The present disclosure provides macrocyclic compounds comprising a 4-amido-2,4-pentadienoate (APD) moiety. The compounds exhibit toxicity that is selective to the hypoxic micro-environments often found in cancerous tissues. The disclosed compounds are therefore suitable for treatment of hypoxic cancer cells.

The present invention relates to use of a chelating compound for chromatographic separation of rare earth elements, actinides, and/or s-, p- and d-block metals, and to a method of chromatographic separation of chelates of rare earth elements, actinides and/or s-, p- and d-block metals from a mixture of at least two metal ions. The method is characterized in that it comprises the following steps: (a) providing a mixture of at least two different metal ions chosen from rare earth metal ions, actinide ions and/or s-, p- and d-block metal ions, (b) contacting metal ions comprised in said mixture to with at least one compound of general formula (I) as defined in any one of the preceding claims to form chelates; (c) subjecting the chelates from step (b) to chromatographic separation, wherein optionally at least one separated metal chelate obtained in step (c) can be subjected to at least one further chromatographic separation in order to increase the purity of the at least one separated metal chelate; and, optionally, (d) obtaining the metal from the at least one separated metal chelate.

The present invention relates to use of a chelating compound for chromatographic separation of rare earth elements, actinides, and/or s-, p- and d-block metals, and to a method of chromatographic separation of chelates of rare earth elements, actinides and/or s-, p- and d-block metals from a mixture of at least two metal ions. The method is characterized in that it comprises the following steps: (a) providing a mixture of at least two different metal ions chosen from rare earth metal ions, actinide ions and/or s-, p- and d-block metal ions, (b) contacting metal ions comprised in said mixture to with at least one compound of general formula (I) as defined in any one of the preceding claims to form chelates; (c) subjecting the chelates from step (b) to chromatographic separation, wherein optionally at least one separated metal chelate obtained in step (c) can be subjected to at least one further chromatographic separation in order to increase the purity of the at least one separated metal chelate; and, optionally, (d) obtaining the metal from the at least one separated metal chelate.

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

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.

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.