biofilm

Ceftazidime (GR20263) is a beta-lactam, cephalosporin antibiotic with bactericidal activity.

Ceftazidime Pentahydrate is a cephalosporin antibiotic with activity against gram-negative bacilli, including Pseudomonas aeruginosa, and is used in the study of infectious diseases.

D-Tyrosine, the D-isomer of tyrosine, acts as a negative regulator of melanin synthesis by inhibiting tyrosinase activity. Furthermore, D-Tyrosine also inhibits biofilm formation and induces the self-dispersal of biofilms, while not affecting bacterial growth.

MAC-545496 is a glycopeptide-resistance-associated protein R (GraR) inhibitor, is an antivirulence agent.

N-Butanoyl-L-homoserine lactone (C4-HSL) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It exhibits antibacterial activity and is employed in antibacterial biofilm[1].

(+)-Magnoflorine (Thalictrin) has sedative and anxiolytic effects, probably mediated by Magnoflorine through a GABAergic mechanism of action. Magnoflorine and Sinomenine have protective effects, are mediated by some mechanism other than prevention of micelle formation or protection of the erythrocyte membrane against osmotic imbalance.

(+)-Magnoflorine iodide (Thalictrine iodide) has anti-inflammatory activity, it can inhibit inflammations.

Usaramine (Mucronatine) demonstrates phytotoxicity against Lactuca sativa var. Carrascoy (lettuce) assessed as inhibition of seed germination at 50 ug/cm2 after 24 hr.

(+)-Magnoflorine chloride (Escholine chloride) has anti-inflammatory activity, it can inhibit inflammations.

(Z)-2-decenoic acid (cis-dec-2-enoic acid) is an unsaturated short-chain fatty acid secreted by Pseudomonas aeruginosa. It can induce a dispersion response in biofilms formed by gram-negative and gram-positive bacteria and can also inhibit biofilm development.

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

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-3 (compound 3b) is a tetraformamide antibacterial compound that effectively inhibits the plant bacterial pathogen Xanthomonas citri ssp. citri (Xcc) with a minimum inhibitory concentration (MIC) of 500 μg/mL. It also suppresses biofilm formation of Xcc, with an IC50 of 15.37 μg/mL.

Antibiofilm agent-5 (compound 6c) is a multitarget antibacterial agent with potent antibiofilm activity. It induces metabolic dysfunction by inactivating lactate dehydrogenase, promoting the accumulation of reactive oxygen species, which subsequently reduces reduced glutathione and leads to bacterial oxidative damage. Antibiofilm agent-5 is applicable for studying recalcitrant biofilm-enhanced bacterial infections.

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.

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

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-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-4 is a LasR inhibitor, demonstrating optimal antibiofilm and anti-QS (quorum sensing) properties.

Antibiofilm agent-6 (Compound 26c) is a quorum sensing inhibitor with antibiofilm properties, effectively reducing the fluorescence intensity of PAO1-lasB-gfp and PAO1-pqsA-gfp in a concentration-dependent manner. It suppresses the production of pyocyanin and rhamnolipids and enhances the efficacy of ciprofloxacin in eradicating viable bacteria in a Pseudomonas aeruginosa (P. aeruginosa PAO1) infected mouse model.

Antibiofilm agent-7 (Compound 9) demonstrates significant antibiofilm activity with IC50 values of 60 µg/mL, 133.32 µg/mL, and 19.67 µg/mL against Staphylococcus aureus, Escherichia coli, and methicillin-resistant Staphylococcus aureus (MRSA), respectively. It also exhibits antimicrobial activity with MIC values of 4.88 µg/mL, 78.13 µg/mL, 9.77 µg/mL, and 39.06 µg/mL against Staphylococcus aureus, Escherichia coli, Candida albicans, and MRSA, respectively.

Antibiofilm agent-8 (compound Ru2) boosts antibacterial activity under visible light (400-700 nm, 10 J cm-2). It induces oxidative stress by promoting NADH oxidation and reactive oxygen species (ROS) generation, which disrupts the bacterial cell wall.

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