p. aeruginosa

Azurin (50-77) is a peptide fragment derived from the copper-containing bacterial protein azurin, present in P. aeruginosa. It exhibits properties that regulate the cell cycle, inhibit cancer proliferation, and manage angiogenesis, proving its potential as an anticancer agent. Specifically, this compound acts as a VEGFR2 inhibitor with an IC20 of approximately 10.7 µM. At a concentration of 20 µM, it effectively induces cell cycle arrest at the G2/M phase in MCF-7 breast cancer cells, while a higher concentration of 50 µM significantly reduces the proliferation of both MCF-7 and ZR-75-1 breast cancer cell lines. Furthermore, Azurin (50-77) impedes VEGF-A-induced capillary tube formation with an IC50 of 12 µM, and alters the cellular and extracellular levels of critical signaling and structural proteins such as F-actin, focal adhesion kinase (FAK), paxillin, and platelet endothelial cell adhesion molecule-1 (PECAM-1) in human umbilical vein endothelial cells (HUVECs) at a concentration of 25 µM. Demonstrating its efficacy in vivo, Azurin (50-77) administered at 10 mg/kg per day notably reduces tumor volume in an MCF-7 mouse xenograft model, highlighting its therapeutic potential.

Lipopolysaccharides from P. aeruginosa (Pseudomonas aeruginosa) 10 are endotoxins and TLR4 activators that originate from the bacterium P. aeruginosa 10, classified as S-type LPS. They exhibit a characteristic tripartite structure: an O antigen, a core oligosaccharide, and lipid A. The lipopolysaccharides from P. aeruginosa 10 are distinct due to their unique fatty acid composition, an unusually high level of phosphorylation (identified as triphosphate residues), and a distinctive outer region in the core oligosaccharide. Moreover, their O-specific side chains are typically rich in novel amino sugars. These lipopolysaccharides display susceptibility to viruses, with their viral sensitivity being influenced by the molecular weight polysaccharide content. A reduction in high-molecular-weight polysaccharides increases their sensitivity to bacteriophages.

Zidebactam (WCK-5107) is an effective β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 inhibitor (IC50: 0.26 μg/mL).

Ceftolozane sulfate (FR-264205) is a cephalosporin antibiotic with broad-spectrum antimicrobial activity, inhibits P. aeruginosa PAO1, inhibits Pseudomonas aeruginosa, and is used in the study of pneumonia.

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg/ml, 4 μg/ml, and 16 μg/ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

Imipenem monohydrate (Imipenem) is a carbapenem antibiotic isolated from the microorganism Streptomyces cattleya, and is a β lactam antibiotic. Imipenem monohydrate acts on the bacterial cell wall, and is a broadly effective inhibitor of a wide range of Gram-positive and negative bacteria.

Adipic dihydrazide (ADH) is a dihydrazide with a symmetrical C4 skeleton, commonly used as a bifunctional cross-linking agent for water-in-oil emulsions and a curing agent for epoxy resins. ADH exhibits antibacterial activity against E. coli and P. aeruginosa.

6-Hydroxynicotinic acid (6-Hydroxypyridine-3-carboxylic acid) is exploited in the use of NMR spectroscopy or gas chromatography--mass spectrometry for the diagnosis of Pseudomonas aeruginosa in urinary tract infection. Among the common bacteria causing urinary infection, only P. aeruginosa produces 6-hydroxynicotinic acid from nicotinic acid.

Moxalactam sodium salt (LY-127935) is an antibiotic compound more effective against Escherichia coli and Pseudomonas aeruginosathan cephalosporins.

ML318 is a biaryl nitrile PvdQ acylase inhibitor (IC50 of 20 nM for binding in the acyl-binding site). ML318 inhibits P. aeruginosa (PAO1) with IC50 of 19 μM. ML318 prevents pyoverdine production and limits the growth of P. aeruginosa under iron-limiting

CysHHC10 acetate shows antibacterial activities against both Gram-positive and Gram-negative bacteria with MIC of 10.1, 20.2, 2.5, and 1.3 mM for E. coli, P. aeruginosa, S. aureus, and S. epidermidis, respectively.

Equisetin, an N-methylserine-derived acyl tetramic acid isolated from the terrestrial fungus Fusarium equiseti NRRL 5537, functions as a Quorum-sensing inhibitor (QSI) that specifically attenuates QS-regulated virulence phenotypes in P. aeruginosa, presenting a potent lead for treating P. aeruginosa infections without hindering bacterial growth. This tetramate-containing natural product possesses antibiotic and cytotoxic properties, effectively inhibiting the growth of Gram-positive bacteria and HIV-1 integrase activity, yet it does not impact Gram-negative bacteria.

Zidebactam sodium salt is a potent inhibitor of β-lactamase, and also is an inhibitor of penicillin-binding protein2 (PBP2)(IC50 of 0.26 μg/mL).

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively, and it reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM[1].

BAL30072 shows MIC90 values of 4 μg/mL for MDR Acinetobacter spp. and 8 μg/mL for MDR P. aeruginosa, respectively[1][2]. BAL-30072, a siderophore sulfactam, is a monocyclic beta-lactam antibiotic, with activity against multiresistant gram-negative bacilli

Temafloxacin (Omniflox) is an antibiotic and antimycobacterial agent. It used to treat lower respiratory tract infections, genital and urinary infections like prostatitis, and skin infections.

Antibacterialagent 253 (compound 7a) is an effective bacterial inhibitor with a minimum inhibitory concentration (MIC) of 1.562 μg/mL against several pathogens, including Pseudomonas aeruginosa (P. aeruginosa), Staphylococcus aureus (S. aureus), Listeria monocytogenes (L. monocytogenes), Bacillus cereus (B. cereus), and Salmonella typhi (S. typhi).

Carbonic anhydrase inhibitor28 (Compound 11) serves as an inhibitor for the Pseudomonas aeruginosa carbonic anhydrase. It exhibits antibacterial activity, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 and 1 μg/mL, respectively, against P. aeruginosa. Carbonic anhydrase inhibitor28 is utilized in research focused on anti-infection applications.

Antibacterialagent 254 (Compound 2) is an antimicrobial agent capable of eradicating 7-day-old P. aeruginosa biofilms at a concentration of 50 μM without affecting bacterial growth. Additionally, Antibacterialagent 254 enhances the efficacy of Ciprofloxacin against P. aeruginosa and upregulates the expression of the matrix-degrading enzyme genes pelA, pslG, and eddA.

Pterin is a pteridine with antibacterial properties, identified in C. croceus. It inhibits the proliferation and biofilm formation of E. coli, P. aeruginosa, and S. mutans. Pterin holds potential for research in cancer and infections.

Antibacterialagent 260 (Compound 4r) exhibits broad-spectrum antibacterial activity, effectively inhibiting P. aeruginosa and S. aureus with a minimum inhibitory concentration (MIC) of 0.0076 μM. Additionally, Antibacterialagent 260 serves as a herbicide, hindering the growth of radish (Raphanus sativus L.) seed roots and stems.

Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.

Antiangiogenic agent 8 (Compound 3m) functions as both an antibacterial agent and an antiangiogenic compound. It shows minimum inhibitory concentrations (MIC) of 16, 8, 4, 16, and 8 μg/mL against E. coli, P. aeruginosa, B. subtilis, S. aureus, and C. glabrata, respectively, with minimum bactericidal concentrations (MBC) ranging from 32 to 64 μg/mL. This compound holds potential for applications in infection control and cardiovascular disease research.

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.