gyrase

Garenoxacin mesylate hydrate (Garenoxacin mesylate [USAN]) with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.

Garenoxacin (BMS284756) is a novel oral des-fluoro(6) quinolone for the treatment of Gram-positive and Gram-negative bacterial infections.

Trovafloxacin is a broad-spectrum fluoroquinolone antibiotic that inhibits the activity of DNA gyrase and topoisomerase IV, enzymes involved in DNA replication. It also acts as an effective and specific inhibitor of the pannexin 1 channel (PANX1, IC50 = 4 μM).

DNA Gyrase-IN-12 (Compound 6d) is an inhibitor of DNA gyrase. It exhibits antibacterial activity with MIC values ranging from 0.031 to 0.0625 μg mL against Vancomycin-Intermediate Staphylococcus aureus (VISA) and Enterococcus faecium.

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 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].

14α-Demethylase DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase DNA Gyrase, exhibiting antibacterial activity.

DNA gyrase Topo IV-IN-1 (Compound 27) is an inhibitor of DNA gyrase and topoisomerase IV with antibacterial properties. It exhibits IC50 values of 11 and 17 nM against the DNA gyrase of Escherichia coli and methicillin-resistant Staphylococcus aureus, respectively, and IC50 values of 83 and 21 nM against topoisomerase IV of the same organisms. DNA gyrase Topo IV-IN-1 is applicable in anti-infective research.

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-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].

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.

DNA Gyrase-IN-13 (compound 1b) is an inhibitor of DNA gyrase with bacteriostatic properties. It exhibits an IC50 of 1.81 μM against Staphylococcus aureus DNA gyrase.

DNA Gyrase-IN-16 (Compound 9) is an inhibitor of DNA gyrase, with an IC50 of 1.609 μM. It exhibits antibacterial properties, effectively inhibiting S. aureus and MRSA, with a MIC of 3.125 μM for both.

DNA Gyrase-IN-7 (compound 6d), a new inhibitor of Microbial DNA-Gyrase, is described in reference [1].

DNA Gyrase-IN-1 is a potent and selective DNA promoter inhibitor (IC50: 2.6 μM). DNA Gyrase-IN-1 inhibits Mycobacterium tuberculosis (Mtb) activity well (MIC: 0.49 μM). DNA Gyrase-IN-1 can be used to study tuberculosis.

Antibacterial agent 138, a benzothiazole inhibitor, targets bacterial DNA gyrase and topoisomerase IV, exhibiting both favorable solubility and plasma protein binding. It demonstrates antibacterial activity against Gram-positive and Gram-negative strains and functions as a dual GyrB and ParE inhibitor [1].

DNA Gyrase-IN-15 (Compound 11) is an antibacterial agent that inhibits both DHPS and DNA gyrase, with IC50 values of 1.73 and 0.07 µM, respectively. It shows antimicrobial activity against Enterococcus faecium (MIC of 15.62 µg mL), Acinetobacter baumannii, Enterobacter (MIC of 7.81 µg mL), Pseudomonas aeruginosa, Klebsiella pneumoniae, and Staphylococcus aureus. Additionally, DNA Gyrase-IN-15 exhibits antibiofilm activity against Enterococcus faecium.

DNA Gyrase DHFR-IN-1 is a dual inhibitor targeting bacterial DNA gyrase and DHFR, with IC50 values of 182 μM and 3.90 μM against E. coli DNA gyrase and DHFR, respectively. This compound exhibits both bactericidal and antifungal activities.

DNA Gyrase-IN-9 (compound 4j), an antibacterial agent, selectively targets DNA gyrase and exhibits a minimum inhibitory concentration (MIC) of 0.5-2 µg mL for Gram-positive bacteria inhibition and a minimum bactericidal concentration (MBC) of 2-8 µg mL for Gram-positive bacteria eradication. Notably, this compound hinders DNA gyrase activity in Staphylococcus aureus with an IC50 of 6.29 µg mL [1].

DNA Gyrase-IN-11 (Compound 23Be) is an inhibitor of protein synthesis (IC50 of 0.74 μM) and DNA replication. It specifically targets and inhibits DNA Gyrase (DNA Gyrase), which suppresses the supercoiling of DNA in E. coli with an IC50 of 11.9 μM. Moreover, DNA Gyrase-IN-11 exhibits antibacterial activity against Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae, and Staphylococcus aureus, with minimum inhibitory concentrations (MIC) ranging from 0.008 to 0.25 μg mL.

DNA Gyrase-IN-8 is a potent DNA gyrase inhibitor, exhibiting antimicrobial activity with an IC50 of 8.45 µM [1].

DNA Gyrase-IN-4 (compound 8p) is a potent inhibitor of DNA cyclooxygenase (IC50: 0.13 μM) and exhibits significant antimicrobial activity with minimum inhibitory concentrations (MIC) of 0.05 μg ml against Salmonella and 8 μg ml against Escherichia coli.

DNA Gyrase-IN-5 is a potent inhibitor of DNA gyrase (IC50: 0.10 μM) and has an antibacterial effect on both wild-type and drug-resistant strains.