Molecules That Inhibit Efflux Pumps in Multi-Drug Resistant Bacteria and Uses Thereof
US-2016361292-A1 · Dec 15, 2016 · US
US12433855B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12433855-B2 |
| Application number | US-201917283471-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 8, 2019 |
| Priority date | Oct 8, 2018 |
| Publication date | Oct 7, 2025 |
| Grant date | Oct 7, 2025 |
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This invention relates to macrocyclic cavity containing compounds and uses thereof in inhibiting a microbial signalling molecule or in reducing the amount of a microbial signalling molecule in a subject. The invention also relates to methods for inhibiting a microbial signalling molecule or for reducing the amount of a microbial signalling molecule in a subject by contacting a macrocyclic cavity-containing compound with said subject.
Opening claim text (preview).
The invention claimed is: 1. A method to inhibit a microbial quorum signalling molecule or to reduce the amount of a microbial quorum signalling molecule produced by a Gram-negative bacteria in a subject, by binding the microbial quorum signaling molecule selected from homoserine lactones (HSLs) or N-acyl homoserine lactones (AHLs) by non-covalent host-guest bonding by a macrocyclic cavity-containing compound, wherein the method comprises contacting the macrocyclic, cavity-containing compound selected from pillar[5]arenes and/or salts thereof with said subject. 2. The method according to claim 1 , wherein the Gram-negative bacteria comprises planktonic microbes. 3. A method to prevent or treat a microbial quorum signalling molecule dependent and/or mediated infection in a subject or a medium, which infection is caused by a Gram-negative bacteria by binding the microbial quorum signaling molecule selected from homoserine lactones (HSLs) or N-acyl homoserine lactones (AHLs) by non-covalent host-guest bonding by a macrocyclic cavity-containing compound, wherein the method comprises contacting the macrocyclic cavity-containing compound selected from pillar[5]arenes and/or salts thereof with said subject or medium. 4. The method according to claim 3 , wherein the infection is an acute infection or the infection is caused by planktonic microbes. 5. A method to reduce or abolish virulence in a Gram-negative bacteria by non-covalent host-guest bonding between a macrocyclic cavity-containing compound and a microbial quorum signaling molecule selected from homoserine lactones (HSLs) or N-acyl homoserine lactones (AHLs) produced by a Gram-negative bacteria, wherein the macrocyclic cavity-containing compound is selected from pillar[5]arenes and/or salts thereof. 6. The method according to claim 5 , wherein the Gram-negative bacteria comprises planktonic microbes.
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327) · CPC title
Cyclodextrins · CPC title
condensed with other heterocyclic ring systems, e.g. biotin, sorbinil · CPC title
having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel · CPC title
Antibacterial agents · CPC title
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