Rela/rsh inhibitors for the treatment or prevention of medical biofilms
AssigneeDrexel University
InventorsDonald Carl Hall, JR., Jaroslaw E. Krol, Hai-Feng Ji, Garth David Ehrlich
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Abstract
Disclosed herein are certain compounds capable of inhibiting bacterial RelA/RSH, and/or minimizing and/or inhibiting formation of bacterial biofilms, and/or compromising and/or reducing integrity of formed biofilms, and/or inhibiting the production of toxins by gram-negative bacteria. Also disclosed herein are methods of inhibiting the formation of and/or compromising and/or reducing integrity of formed biofilms, as well as methods of inhibiting production of toxins by gram-negative bacteria using the compounds disclosed herein.
Claims22
A method of treating, ameliorating, or preventing biofilm formation by a bacterium, the method comprising contacting the bacterium with at least one compound selected from
- (a) a compound of Formula I:
- or a salt, solvate, tautomer, N-oxide, geometric isomer, stereoisomer thereof, or mixtures thereof, wherein:
- R1 is —NH— or —O—,
- R2 is —CH2— or —C(O)—,
- A is a five member aromatic heterocyclic ring or —CH═CH—COO—*, wherein * is the bond to R3.
- R3 is —O—C(O)OH or
- and
- R4 and R5 are each independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, or —OH;
- (b)
- 3-(3-(4-bromo-1H-pyrazol-1-yl)benzamido)propanoic acid (C22), or a salt, solvate, tautomer, N-oxide, geometric isomer, or mixtures thereof.
(canceled)
A method of inhibiting toxin production by a gram-negative bacterium, the method comprising contacting the gram-negative bacterium with at least one compound selected from:
- (a) a compound of Formula I:
- or a salt, solvate, tautomer, N-oxide, geometric isomer, stereoisomer thereof, or mixtures thereof, wherein:
- R1 is —NH— or —O—,
- R2 is —CH2— or —C(O)—,
- A is a five member aromatic heterocyclic ring or —CH═CH—COO—*, wherein * is the bond to R3.
- R3 is —O—C(O)OH or
- and
- R4 and R5 are each independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, or —OH;
- (b)
- 3-(3-(4-bromo-1H-pyrazol-1-yl)benzamido)propanoic acid (C22), or a salt, solvate, tautomer, N-oxide, geometric isomer, or mixtures thereof.
(canceled)
A compound of Formula I:
- or a salt, solvate, tautomer, N-oxide, geometric isomer, stereoisomer thereof, or mixtures thereof,
- wherein:
- R1 is —NH— or —O—,
- R2 is —CH2— or —C(O)—,
- A is a five member aromatic heterocyclic ring or —CH═CH—COO—*, wherein * is the bond to R3.
- R3 is —O—C(O)OH or
- R4 and R5 are each independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, or —OH,
- with the proviso that the compound is not
- 2-(4-((2,5-dioxoimidazolidin-4-yl)methyl)-1H-1,2,3-triazol-1-yl)acetic acid.
Dependencies are inferred from the claim text.