gyrase

Enoxacin hydrate (AT-2266 hydrate) is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.

Enoxacin (NSC-629661) is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent (fluoroquinolones) structurally related to nalidixic acid.

Trovafloxacin, a broad-spectrum quinolone antibiotic, exhibits potent activity against Gram-positive bacteria.

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).

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

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

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-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/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/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.

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-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.

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-IN-17 (Compound 5C) is an inhibitor of DNA gyrase. It demonstrates significant antimicrobial activity against a range of Gram-positive and Gram-negative strains, including Enterococcus faecium, Escherichia coli, and Pseudomonas aeruginosa, with a MIC value of 62.5 μg/mL. By inhibiting bacterial DNA gyrase, DNA Gyrase-IN-17 disrupts DNA replication. This compound can be useful in the development of antibiotics, particularly for studying resistant strains.

DNA Gyrase-IN-10 is a potent inhibitor of DNA gyrase, exhibiting strong antibacterial activity. It effectively inhibits both Gram-positive and Gram-negative bacteria.

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.

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.

14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase and DNA Gyrase, exhibiting significant antibacterial activity.

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

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.

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-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.

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).