gyrase b

E.coli Gyrase B-IN-1 (Compound 10g) is an inhibitor of E.coli Gyrase B, demonstrating antibacterial properties. It exhibits potent inhibitory activity against Escherichia coli (E. coli) with a minimum inhibitory concentration (MIC) of 0.12 mM. E.coli Gyrase B-IN-1 shows promise for research in antibacterial agents.

DNA gyrase B-IN-1 is a potent inhibitor of DNA gyrase B, exhibiting good binding affinity and stability. DNA gyrase B-IN-1 inhibits P. aeruginosa/i> DNA gyrase B (IC50: 2.2 μM).

DNA gyrase B-IN-3 (Compound A), with an IC50 of less than 10 nM, functions as an inhibitor of bacterial DNA gyrase B and demonstrates antibacterial activity against Gram-positive strains [1].

DNA gyrase B-IN-2 (Compound E), a 2-aminobenzothiazole derivative, serves as a potent inhibitor of DNA gyrase B with substantial efficacy against ESKAPE pathogens. It demonstrates nanomolar-range inhibition (IC 50 < 10 nM) and a broad-spectrum antibacterial effect, with minimum inhibitory concentrations below 0.03 μg/mL for most Gram-positive species and between 4–16 μg/mL for Gram-negative species including E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae. DNA gyrase B-IN-2 is applicable in infection research [1].

SPR719 is an inhibitor of gyrase B, has bactericidal activity.

DNA gyrase/Topo IV-IN-2 (Compound AK19) is an antibacterial agent with IC50 values of 0.783 μM and 7.136 μM for inhibiting E. coli DNA gyrase and topoisomerase IV, respectively. It exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative pathogens and inhibits biofilm formation in B. subtilis and MRSA, with a MIC of 1.9 μM. DNA gyrase/Topo IV-IN-2 is useful for researching drugs targeting resistant bacteria.

Flumequine-13C3 is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine (T1060) is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae (MICs = 1-100 μg/ml). Flumequine (T1060) is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3

Dihydronovobiocin is a coumarin antibiotic and derivative of novobiocin .1It is active against the bacteriaS. aureus,S. haemolyticus,D. pneumoniae,S. typhosa,K. pneumoniae, andP. multocida(MICs = 0.6, 2, 0.6, 10, 10, and 3 μg/ml, respectively).2Dihydronovobiocin inhibits DNA gyrase subunit B with an IC50value of 64.5 nM.3 1.Berger, J., and Batcho, A.D.Coumarin - glycoside antibioticsJ. Chromatogr. Lib.15101-158(1978) 2.Hoeksema, H.Dihydronovobiocin and derivatives thereof3,175,9441-9(1965) 3.Gevi, M., and Domenici, E.A scintillation proximity assay amenable for screening and characterization of DNA gyrase B subunit inhibitorsAnal. Biochem.300(1)34-39(2002)

Antibacterial agent 98 (compound g37) is an effective oral antibacterial agent that inhibits the ATPase activity of Gyrase B and weakens the DNA super-helix of S. aureus. Notably, it does not induce the development of MRSA (methicillin-resistant Staphylococcus aureus) resistance.

DNA Gyrase-IN-3 (Compound 28) is an inhibitor of bacterial DNA gyrase B with an IC50 of 5.41-15.64 μM for inhibiting Escherichia coli DNA rotatase. It exhibits both anti-tuberculosis and antibacterial activity.

DNA Gyrase-IN-2 is a bacterial DNA cyclooxygenase B inhibitor that acts on Escherichia coli DNA cyclooxygenase (IC50: 3.29-10.49 μM) and Mycobacterium tuberculosis DNA cyclooxygenase (IC50: 4.41-5.61 μM), exhibiting antibacterial and antitubercular effects.

QSL-304 is a DNA gyrase B inhibitor that serves as an antibacterial agent, exhibiting an IC50 of 31.23 mg/mL against Staphylococcus aureus SA-P2003 [1].

Zoliflodacin (ETX0914) (ETX0914, AZD0914) is a new bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus (MIC90: 0.25 μg/mL).

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.