Antibactérien

InhA-IN-7 (Compound 11), a derivative of Triclocan, shows inhibitory activity against enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. It effectively inhibits the proliferation of both wildtype and mutant strains of Mycobacterium tuberculosis, exhibiting minimum inhibitory concentrations (MICs) ranging from 19 to 75 μM [1].

PptT-IN-2 inhibits PptT enzyme crucial in tuberculosis, with 2.5 μM IC50, showing potential in TB research.

KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.

Compound 11: Sulfonylurea derivative, antimicrobial, anticancer; MIC 0.039-0.156 mg/mL; A549 IC50: 19.7 μg/mL, PC3 IC50: 11.9 μg/mL.

Kalafungin inhibits various fungi, yeasts, protozoa, and gram-positive bacteria, less so for gram-negative bacteria.

Glutamate-5-kinase-IN-1 is a potent G5K inhibitor with a 4.1 μM MIC, showing promise in anti-TB research.

MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.

Alpibectir has antibacterial activity [1].

Enzyme-IN-3 disodium (compound 7) is a selective inhibitor of Mycobacterium tuberculosis shikimate kinase with an IC50 of 1.6 μM. Additionally, Enzyme-IN-3 disodium exhibits antibacterial properties.

Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.

β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).

Compound 112: Powerful antibacterial, MIC 1250 μM against B. subtilis, E. coli, E. faecalis, S. typhimurium, S. aureus; also an HIV-1 antibody.

Gepotidacin (GSK-2140944) is a potent DNA topoisomerase inhibitor, a novel antibacterial efficacious against various anaerobes.

NBTI 5463 is a bacterial type II topoisomerase (topoisomerase II) inhibitor with antimicrobial properties. It effectively inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. By binding to topoisomerase II, NBTI 5463 prevents DNA cleavage and re-ligation, thereby impeding bacterial DNA replication and transcription. This compound shows potential for research into Gram-negative bacterial infections.

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.

Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is an activator of hydroxycarboxylic acid receptor 1 (HCAR1) and an epigenetic regulator that induces lysine residue lactylation. As the end product of glycolysis, it bridges the gap between glycolysis and oxidative phosphorylation. This compound is a tumor metabolite, offering immunoprotective effects of lactate in antitumor immunity. Additionally, it possesses antimicrobial properties and can be used as a food preservative.

MraY-IN-3 (12a) is a potent inhibitor of the bacterial translocase MraY (IC50: 140 μM). 46 μg/ml).

Metallo-β-lactamase-IN-13 (Compound 13i) serves as a pan Metallo-β-Lactamase inhibitor with extended activity against Gram-negative (GN) bacteria expressing metallo-β-lactamases. It exhibits antibacterial properties effective against P. aeruginosa [1].

AVE-1330A sodium is a beta-Lactamase inhibitor.

LY 215890 is a compound that exhibits potent Gram-negative and Gram-positive antibacterial activity.