Antibacteriano

PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.

Apalcillin (PC-904) combined with Ro 48-1220 (a penicillin sulfone β-lactamase inhibitor) exhibits broad-spectrum activity against Gram-negative aerobic and anaerobic bacteria, excluding Klebsiella acid-producing strains. This combination shows strong efficacy against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae with an effective MIC of 11 μg/mL. Additionally, it inhibits Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter at low MICs (0.25 to 4 μg/mL). However, it has limited efficacy against oxacillin-resistant staphylococci and some Gram-positive bacteria. Apalcillin/Ro 48-1220's effectiveness against certain extended-spectrum β-lactamase-producing Escherichia coli is comparable to piperacillin/tazobactam, though it is less effective against SHV-type β-lactamases.

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

Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.

Antibacterial agent 76 (compound 9) is a potent antibacterial agent.

<p>ROS inducer 9 (compound 4e) is an antibacterial agent with a minimum inhibitory concentration (MIC) of 0.25 μg/mL against Escherichia coli. It eradicates bacteria by inhibiting GSH activity and increasing ROS levels. Additionally, ROS inducer 9 exhibits low toxicity toward red blood cells and RAW 264.7 cells.</p>

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

<p>BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.</p>

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

FG-2101 is a selective, orally active non-hydroxamate LpxC inhibitor with an IC50 of approximately 1 nM. It demonstrates exceptional selectivity over other bacterial and human metalloproteases. FG-2101 is useful for studying infections caused by Gram-negative bacteria, including resistant strains.

Antibacterial agent 77 (compound 12) is an antibacterial agent [1].

Metallo-β-lactamase-IN-16 (compound 18), a sulfone-containing metallo-β-lactamase inhibitor, exhibits antimicrobial activity. It effectively inhibits various metallo-β-lactamases, including NDM-1 (New Delhi metallo-β-lactamase-1), IMP-1 (imipenemase-1), VIM-1 (Verona Integron-encoded Metallo-β-lactamase), and VIM-2. The IC50 values for these enzymes are 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM respectively.

Trans-Clopenthixol ((E)-Clopenthixol) is an antibiotic without any sedative properties. It can be used in vitro to inhibit Pseudomonas aeruginosa and Plasmodium falciparum.

Antibacterialagent 266 (Compound C5) is an inhibitor of plant pathogenic bacteria that disrupts the integrity of bacterial cell membranes. It exhibits an EC50 of 24.1 μg/mL against Xanthomonasoryzaepvoryzae (Xoo) and 39.0 μg/mL against X. axonopodispvcitri (Xac). Antibacterialagent 266 is valuable for research in plant pathology and the development of agricultural antibacterial agents.

LasR-IN-2 blocks LasR via H-bond with TRY-56, useful in bacterial infection and CF research.

<p>9-tert-Butyldoxycycline exhibits immunomodulatory activity by altering the polarization state of polymorphonuclear neutrophils and ameliorating inflammatory responses in ischemia-reperfusion injury models. Additionally, 9-tert-Butyldoxycycline serves as a ligand for the "Tet-On" inducible gene expression system.</p>

GSK656 (GSK3036656) inhibits Mtb LeuRS with IC50 of 0.20 μM, promising for tuberculosis treatment.

PptT-IN-3 (5p), an inhibitor of PptT in Mycobacterium tuberculosis, IC50=3.5μM, is key for TB research.

Benzisothiazolone is an isothiazolinone fungicide that demonstrates growth inhibitory activity against Escherichia coli ATCC 8739 and yeast NCYC 1354. It is utilized in studies investigating growth inhibition models.

MtTMPK-IN-5 inhibits Mtb TMPK with IC50 of 34 μM and fights tuberculosis with MIC of 12.5 μM, aiding TB research.