antibiofilm

Antibiofilm agent-13 (compound 14b) is an effective broad-spectrum antibacterial agent that functions by disrupting the integrity of bacterial cell membranes. It achieves this through the degradation of transmembrane potential and increased membrane permeability, which leads to the production of intracellular ROS and the leakage of DNA and proteins, ultimately resulting in bacterial death. Antibiofilm agent-13 effectively inhibits both Gram-positive bacteria (MIC ranging from 0.5-1 μg mL) and Gram-negative bacteria (MIC ranging from 1-32 μg mL).

Antibiofilm agent prodrug 1 (Compound 5c) demonstrates antibacterial properties by inhibiting biofilm formation and iron uptake. It effectively suppresses Pseudomonas aeruginosa PAO1 with a minimum inhibitory concentration (MIC) of 1.07 μM. In addition, Antibiofilm agent prodrug 1 exhibits anti-infective activity in Caenorhabditis elegans, enhancing the survival rate of the nematodes.

Antibiofilm agent-15 (Compound 17) is an antimicrobial agent that inhibits biofilm formation of both Gram-positive and Gram-negative bacteria.

Antibiofilm agent-14 (compound 11) functions as an antibiofilm agent. It exhibits antifungal activity against C.albicans SC5314, with a minimum inhibitory concentration (MIC) of 50 μM.

Antibiofilm agent-11 (compound C12) is a flavonoid derivative with antibiofilm activity.

Antibiofilm agent-9 (Compound 4), a derivative of pyrrolnitrin, exhibits antimicrobial activity. It inhibits Bacillus anthracis with a Minimum Inhibitory Concentration (MIC) of 0.031 μg mL. The compound demonstrates significant antibiofilm activity, achieving an inhibition rate of 84% after 24 hours at a concentration of 8.0 μg mL. Additionally, Antibiofilm agent-9 shows favorable pharmacokinetic properties in mouse models.

Antibiofilm Agent-1, as detailed in WO2017011725A1 (compound 17) [1], serves as an antibacterial agent effective against Gram-positive pathogens.

Antibiofilm Agent-2 (Compound 4T) serves as a potent biofilm inhibitor, exhibiting an IC50 of 3.6 μM, and impairs the quorum sensing system along with iron homeostasis, acting as antibacterial synergists against Pseudomonas aeruginosa [1].

Antibiofilm agent-12 (Compound C13), an antifungal belonging to the carbamate derivatives, exhibits significant antifungal activity against Candida auris, with an MIC90 of 237.9 μM. It inhibits the drug efflux pump activity of Candida auris and promotes ergosterol depletion, thereby hindering the formation of Candida auris biofilms and reducing its metabolic flexibility. Additionally, Antibiofilm agent-12 demonstrates antifungal efficacy in a C. elegans model following Candida auris infection.

Tridecanoic acid (Tridecylic Acid) is a 13-carbon saturated fatty acid found in dairy products and also as a product of anaerobic biodegradation of n-hexadecane. It has been identified as a substrate of phospholipase A2.

Trans-2,3,4-Trimethoxycinnamic acid, a natural derivative of cinnamic acid, competitively inhibits the binding of 3-oxo-C8-HSL to TraR and exhibits good antitoxic activity and antibiofilm activity against Escherichia coli.

Terpinen-4-ol can be used as an antibacterial and antibiofilm agent against Staphylococcus aureus.

MurA-IN-5 (compound 4c) demonstrates a minimum inhibitory concentration (MIC) of 1.95 μg mL against Escherichia coli and exhibits significant potency as a MurA inhibitor with an IC50 of 3.77 μg mL. It also shows antibiofilm activity against various microorganisms, indicating its potential in combating biofilm-related infections.

Hamamelitannin has cytotoxic, and antibiofilm activities. It increases the susceptibility of S. aureus to antibiotic treatment in in vivo Caenorhabditis elegans and mouse mammary gland infection models. It also has a high protective activity on cell damag

(±)-ε-Viniferin, a racemate of ε-Viniferin, exhibits P450 inhibitory antioxidants, along with hepato-protective and antimicrobial activities. It also demonstrates antibacterial and antibiofilm activities against Gram-positive bacteria Streptococcus pneumoniae, with a minimum inhibitory concentration (MIC) of 20 μM [1].

Hordenine hydrochloride is a biochemical that inhibits the activity of PDK3, inhibits quorum sensing, and acts as an antibiofilm agent against bacteria.

DNA Gyrase-IN-15 (Compound 11) is an antibacterial agent that inhibits both DHPS and DNA gyrase, with IC50 values of 1.73 and 0.07 µM, respectively. It shows antimicrobial activity against Enterococcus faecium (MIC of 15.62 µg mL), Acinetobacter baumannii, Enterobacter (MIC of 7.81 µg mL), Pseudomonas aeruginosa, Klebsiella pneumoniae, and Staphylococcus aureus. Additionally, DNA Gyrase-IN-15 exhibits antibiofilm activity against Enterococcus faecium.

Temporin-GHc exhibits antibacterial activity with an MBIC50 of 6 μM and antibiofilm activity with an MBEC50 of 25 μM at 24 h [1].

Quorum sensing-IN-8 (compound 5e) exhibits antibiofilm activity and can be used in research on antibiotic resistance.

Antibacterial agent 106 (compound 8) is a highly effective orally active antibacterial compound with antibiofilm activity, demonstrating potent antibacterial effects against multi-drug resistant (MDR) Gram-positive pathogens, including the eradication of 99.7% of intracellular methicillin-resistant S. aureus (MRSA) harbored within macrophages [1].

Hordenine sulfate inhibits the activity of PDK3, inhibits quorum sensing, and acts as an antibiofilm agent against bacteria.

L-K6L9 exhibits antimicrobial and antibiofilm properties effective against P. aeruginosa associated with cystic fibrosis, demonstrating both stability and resistance to degradation by sputum proteases from cystic fibrosis patients, without inducing bacterial resistance [1].

D-K6L9 exhibits antimicrobial and antibiofilm properties effective against Pseudomonas aeruginosa isolated from patients with cystic fibrosis. The compound demonstrates stability and resistance to degradation by proteases found in cystic fibrosis sputum and does not promote bacterial resistance [1].

β-Nor-lapachone is an antibiofilm agent of Candida glabrata with antifungal activity [1]. It stimulates ROS production, inhibits efflux activity, adhesion, biofilm formation, and disrupts the metabolism of mature biofilms.