Antibacteriano

DNA Gyrase-IN-1: potent, selective promoter inhibitor. IC50: 2.6 μM, inhibits Mtb, MIC: 0.49 μM. Useful for tuberculosis 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.

Colistin adjuvant-1, inhibits NF-κB (IC50: 0.209 μM), boosts mucin against gram-negative bacteria.

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).

TBAJ-5307 is a broad-spectrum anti-non-tuberculous mycobacteria inhibitor that targets the FO-domain of the engine, preventing rotation and proton-translocation. TBAJ-5307 inhibits non-tuberculous mycobacteria in vitro and in vivo [1].

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.

Alpibectir has antibacterial activity [1].

Aurachin C is a quinoline alkaloid belonging to the isoprenoid class, known for its antimalarial, antifungal, and antibacterial properties. It acts as a selective terminal oxidase inhibitor.

Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.

844-TFM, a NBTI DNA gyrase blocker, IC50: 1.5 μM, kills Mycobacterium abscessus.

<p>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.</p>

(S)-ZG197 is a compound that acts as a highly selective activator of the Staphylococcus aureus Caseinolytic Protease P (Sa ClpP), demonstrating efficacy at a

OPC-167832: oral dprE1 inhibitor, IC50 0.258 μM, anti-tuberculosis, for Mycobacterium tuberculosis research.

PqsR-IN-1, potent PqsR inhibitor, curbs pyocyanin in Pseudomonas aeruginosa with low cytotoxicity.

MtTMPK-IN-8 inhibits MtbTMPK, has low cytotoxicity, shows 0.78-9.4 μM activity against Mycobacterium, useful for tuberculosis research.

HC2210 exhibits antibacterial effects against Mycobacterium abscessus (Mab) with an EC50 of 0.72 µM. It modulates the expression of Mab genes associated with oxidative stress and lipid metabolism. HC2210 is applicable for studies on Mab infections.

<p>Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg/mL, and exhibits anti-tuberculosis activity.</p>

<p>Mt KARI-IN-1 inhibits Mtb KARI with a 3.06 μM Ki, targeting tuberculosis.</p>

TAN-1057C is a potent antibiotic with antimicrobial activity against both Gram-negative and Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus (MRSA).