Substituted Tolans for the Modulation of Microbial Colonization
AssigneeBioMendics, LLC
InventorsKaren M. McGuire, Chun-che Tsai, Emily L. Plocinik, Aleesha M. McCormick
Life of this patent
Estimating the term…
Loading patent…
AssigneeBioMendics, LLC
InventorsKaren M. McGuire, Chun-che Tsai, Emily L. Plocinik, Aleesha M. McCormick
Estimating the term…
Described are methods for disinfecting a physical or biological surface by contact with an antimicrobial formulation comprising a substituted tolan compound, the substitutions being, for example, one or more alkoxy, (e.g., methoxy) and hydroxy substituents at one or both phenyl rings of the tolan. The compounds and methods are -static and/or -cidal, depending on dose and suspected microbe. Suspected pathogenic microbes include Gram negative bacteria, such as P. aeruginosa and E. coli, Gram positive bacteria, such as S. aureus, including MRSA, and fungal pathogens, such as Candida genus and C. albicans. Also described are methods for inhibiting or disrupting biofilm formation of a microbe or microbes.
A method for inhibiting growth of, or killing, suspected pathogenic microbes on a physical or biological surface, comprising contacting the physical or biological surface with an antimicrobial formulation comprising:
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the tolan is a methoxy tolan.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein at least one of R1 and R2 is hydroxy.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein R1 a is —(C1-C6) alkoxy and m is 1 or 2.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein R2 is hydroxyl and n is 1, 2, or 3.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the substituted tolan is selected from 4,4′-dihydroxytolan, 4,4′-dihydroxy-3-methoxytolan, 4-hydroxy-4′-methoxytolan, 3,5,3′,5′ tetrahydroxytolan, 2,4,4′-trimethoxytolan, 3,5,3′,5′ tetramethoxytolan, and 4-hydroxy-4′-trifluoromethyltolan.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the substituted tolan compound is present in an amount from about 0.01% to about 30% by weight, based on total weight of the antimicrobial formulation.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the antimicrobial formulation has a pH of from about 4.1 to about 8.5, and wherein the antimicrobial formulation further includes a cleansing agent and a secondary antimicrobial agent.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the surface is a physical surface selected from surgical equipment, surgical instruments, and countertop surfaces that must be sterilized and remain sterile throughout a surgical procedure.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the surface is a physical surface selected from food preparation surfaces selected from cutting boards, countertops, and cookware.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the surface is a biological surface at a site where skin is not fully intact, the site selected from intravenous lines or ports, arterial lines or ports, PICC lines, catheters, drains, and incision sites.
The method of claim 1 or 26, or the use of claim 42 or 44, further comprising disrupting a bacterial biofilm in situ.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the surface is a human biological surface selected from skin, scalp, hair, eyes, mucous membranes, and internal or external orifices.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the suspected pathogenic microbes are Gram-negative bacteria.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the suspected pathogenic microbes are Gram-positive bacteria.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the suspected pathogenic microbes are fungi.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the suspected pathogenic microbes are bacterial pathogens selected from methicillin resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, Acinetobacter baumannii, and E. coli species.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the suspected pathogenic microbes are fungi of the Candida genus.
The method of claim 1 or 26, or the use of claim 42 or 44, wherein the antimicrobial formulation further comprises an antibiotic, or wherein the physical or biological surface is further contacted with the antibiotic.
A method of inhibiting or disrupting biofilm formation of a microbe or microbes, the method comprising contacting the microbe or microbes with an antimicrobial formulation comprising:
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound is present in the antimicrobial formulation at a concentration ranging from about 0.008 mM to about 1 mM.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound is present in the antimicrobial formulation at a concentration of about 0.625 mM.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound is present in the antimicrobial formulation in an amount ranging from about 0.0001% to about 30% by weight, based on total weight of the antimicrobial formulation.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound is present in the antimicrobial formulation in an amount ranging from about 0.01% to about 25% by weight, based on total weight of the antimicrobial formulation.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound is present in the antimicrobial formulation in an amount ranging from about 0.1% to about 30% by weight, based on total weight of the antimicrobial formulation.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the antimicrobial formulation is administered from once daily up to about 6 times per day.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the antimicrobial formulation is administered via an administration route selected from the group consisting of topical, transdermal, oral, nasal, ophthalmic, otic, intravenous, intramuscular, subcutaneous, rectal, and vaginal.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the tolan compound comprises 4-hydroxy-4′-methoxytolan.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the microbe or microbes comprise Gram-positive bacteria.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the microbe or microbes comprise Gram-negative bacteria.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the microbe or microbes comprise a fungi.
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the microbe or microbes comprise methicillin resistant Staphylococcus aureus (MRSA).
The method of claim 26 or 1, or the use of claim 42 or 44, wherein the antimicrobial formulation further comprises an antibiotic, or wherein the microbe or microbes are further contacted with the antibiotic.
Use of a substituted tolan compound having the structure (I) in the manufacture of an antimicrobial formulation:
Use of a substituted tolan compound having the structure (I) in the manufacture of a biofilm-disrupting agent:
Dependencies are inferred from the claim text.