Inhibition of two-component signal transduction systems
OwnerDacre England, Staffan Kjelleberginventors
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Abstract
The present invention provides compositions and methods for inhibition activities and actions of microorganisms, particularly bacteria The compositions and methods are based primarily on the inhibition of two-component signal transduction systems with hologenated furanones and related 3-haloalkenones.
Claims26
A composition for use in inhibiting at least one phenotype of a microorganism. the cormposition comprising at least one compound of general formula I:
- 18
- wherein R1 and R2 are independently H, halogen, alkyl, alkoxy, oxcalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more heteroatoms, straight chain or branched chain, hydrophilic or fluorophilic,
- R3 and R4 are independently H. halogen, alkyl, aryl or arylalkyl, alkoxy, alkylsilyl;
- R3 or R4+R2 can be a saturated or an unsaturated cycloalkane;
- and “---” represents a single bond or a double bond provided that at least one of R1, R2, R3 and R4 is halogen and where R3=H and R4=Ph, R1 and R2 can independently be H, halogen, alkyl, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optLonally interrupted by one or more heteroatoms, straight chain or branched chain, hydrophilic or fluorophilic,
- or a compound of general formula II
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- wherein R6 and R7 are independently H. halogen, carboxyl, ester, formyl, cyano, alkyl. alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more beteroatoms, straight chain or branched chain, hydrophilic or fluorophilic;
- X is a halogen;
- R5 is H. alkyl, alkenyl, alkynyl. alkene, alkyne. aryl, arylalkyl, whether unsubstituted or substituted, optionally interrupted by one or more heteroatoms, straight chain or branched chain, hydrophilic or fluorophilic.
A method of inhibiting at least one phenotype of a rnicroorgaism, the method comprising exposing the microorganism to a composition comprising at least one compound of general formula I:
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- wherein R1 and R2 are independently H, halogen, alkyl, alkoxy, oxoalky, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more heteroatorns, straight chain or branched chain, hydrophilic or fluorophilic;
- R3 and R4 are independently H, halogen, alkyl. aryl or arylalk, alkoxy, alkylsilyl,
- R3 or R4+R2 can be a saturated or an unsaturated cycloalkane;
- and “---” represents a single bond or a double bond provided that at least one of R1, R2, R3 and R4 is halogen and where R3=H and R4=Ph, R1 and R2 can independently be H, halogen, alky, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted. optionally interrupted by one or more heteroatoms, straight chain or branched chain, hydrophilic or fluorophilic;
- or a compound of general formula II
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- wherein R8 and R7 are independently H, halogen, carboxyl, ester, formyl, cyano, ale, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more heteroatoms, straight chain or branched chain, hydrophilic or fluorophilic;
- X is a halogen;
- R5 is H. alkyl, alkenyl, alkynyl, alkene, alkyne, aryl, arylalkyl, whether unsubstituted or substituted, optionally interrupted by one or more beteroatorns, straight chain or branched chain, hydrophilic or fluorophilic,
Dependencies are inferred from the claim text.