Antibacterial agent 352
Antibacterial agent 352 is an orally active Antibacterial agent. Antibacterial agent 352 binds to the active cavity of Staphylococcus aureus DNA gyrase via hydrogen bonding, π-π stacking and hydrophobic interactions, thereby blocking bacterial DNA synthesis. Antibacterial agent 352 exhibits antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus pumilus, Staphylococcus epidermidis and Enterococcus faecalis. Antibacterial agent 352 can disrupt established Staphylococcus aureus biofilms and inhibit the formation of Staphylococcus aureus biofilms. Antibacterial agent 352 can be used in the research of Staphylococcus aureus wound infections.
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- Formule: C22H16ClN3O5
- Masse moléculaire:437.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
DNA Gyrase |
In Vitro
Antibacterial agent 352 (Compound W-2-4) (24 h) potently inhibits the growth of S. aureus ATCC 6538 (MIC = 2 μg/mL), B. pumilus AS1.212 (MIC = 2 μg/mL), S. epidermidis ATCC122228 (MIC = 4 μg/mL), and E. faecium AS1.130 (MIC = 0.5 μg/mL) in vitro[1].
Antibacterial agent 352 (1-8 μg/mL; 24 h) acts as a bactericidal agent against S. aureus ATCC 6538 with an MBC of 8 μg/mL (MBC/MIC ratio = 4)[1].
Antibacterial agent 352 (20-400 μg/mL; 3 h) disrupts the membrane integrity of S. aureus ATCC 6538, causing concentration- and time-dependent leakage of intracellular proteins[1].
Antibacterial agent 352 (0.5-8 μg/mL; 24 h) disrupts pre-formed S. aureus ATCC 6538 biofilms in a concentration-dependent manner, achieving a 67.9% clearance rate at 8 μg/mL (4×MIC)[1].
Antibacterial agent 352 (1.2-100.0 μg/mL; 72 h) has low cytotoxicity against HaCaT and H1975 cells, with IC50 values greater than 100 μM, resulting in a selectivity index greater than 19.9 against S. aureus ATCC 6538[1].
Antibacterial agent 352 (8-512 μg/mL; 1 h) exhibits minimal hemolytic activity against sheep erythrocytes, with hemolysis rates below 7% even at concentrations up to 512 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Antibacterial agent 352 (30-60 mg/kg; p.o.; daily; for 7 consecutive days) shows no significant acute systemic toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM mice (female, 4-5 weeks old, SPF-grade)[1]
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Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg
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Administration:p.o.; every other day; 6 doses
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Result:Accelerated wound healing compared to the saline control at 12 days post-treatment.
Reduced bacterial burden in wound tissue by one-log (≈300 CFU at 104 dilution, vs. ≈3000 CFU in the control) at 10 mg/kg dose at 12 days post-treatment.
Achieved a wound healing rate of ≈94.73% (comparable to vancomycin 20 mg/kg) at 20 mg/kg dose at 12 days post-treatment.
Reduced bacterial burden by two-log (17 CFU at 104 dilution) at 20 mg/kg dose at 12 days post-treatment.
Resulted in complete wound healing at 30 mg/kg dose at 12 days post-treatment.
Eradicated all S. aureus from wound tissue (no bacterial colonies recovered) at 30 mg/kg dose at 12 days post-treatment.
Reduced inflammatory cell infiltration, preserved intact tissue structure, and showed regularly arranged collagen fibers (resembling normal tissue) via histopathological analysis at 30 mg/kg dose.
Chemical Information
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Masse moléculaire 437.83
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Formule C22H16ClN3O5
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SMILES
O=C(O)CCN(C(C1=CC=C(N/N=C/C2=CC(Cl)=CC=C2O)C3=CC=CC4=C13)=O)C4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antibacterial agent 352 Related Classifications
HY-184287 Related Classifications
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