gyrase

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

DNA Gyrase-IN-3 (Compound 28) is an inhibitor of bacterial DNA gyrase B. The IC50 of DNA Gyrase-IN-3 inhibits Escherichia coli DNA rotatase is 5.41-15.64 μM. DNA Gyrase-IN-3 shows anti-tuberculosis and antibacterial activity.

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

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-9 (compound 4j), an antibacterial agent, selectively targets DNA gyrase. It 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-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].

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.

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

DNA Gyrase-IN-4 (compound 8p) is a potent inhibitor of DNA cyclooxygenase (IC50: 0.13 μM). (MIC: 0.05 μg/ml), Salmonella (MIC: 0.05 μg/ml) and Escherichia coli (MIC: 8 μg/ml).

Danofloxacin mesylate (CP 76136-27) is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase.

Alalevonadifloxacin is a DNA gyrase and DNA topoisomerase inhibitor and a novel antibacterial compound of the quinolone class targeting MRSa. Alalevonadifloxacin is potentially useful in the treatment of bacterial Gram-positive, Gram-negative and anaerobic infections.

Tosufloxacin hydrochloride is a fluoroquinolone antibacterial agent used to treat bacterial infections.Tosufloxacin hydrochloride is also a bacterial Topo (DNA gyrase, topoisomerase)) inhibitor.

Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.

Finafloxacin, a fluoroquinolone antimicrobial agent from a new 8-cyano subclass, is most effective in slightly acidic environments (pH 5.0-6.0), a condition where other fluoroquinolones typically reduce in activity. It selectively targets bacterial type II topoisomerases, such as DNA gyrase and DNA topoisomerase IV, making it suitable for treating serious bacterial infections particularly in acidic contexts, including urinary tract infections (UTIs) and Helicobacter pylori infections.

Ofloxacin (Oxaldin) is a fluoroquinolone antibacterial antibiotic. Ofloxacin binds to and inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes involved in DNA replication and repair, resulting in cell death in sensitive bacterial species.

Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

Albicidin is a DNA gyrase inhibitor produced by Xanthomonas albilineans.

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

Pefloxacin Mesylate Dihydrate (1589 RB) , an antibacterial agent, restrains bacterial DNA replication by inhibiting DNA gyrase (topoisomerase).

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine 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 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.3In vivo, flumequine (50 mg/kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

Clorobiocin is an aminocoumarin antibacterial that suppresses the enzyme DNA gyrase.

Evybactin, a DNA gyrase inhibitor, selectively targets Mycobacterium tuberculosis, demonstrating a minimum inhibitory concentration (MIC) value of 0.25 µg/mL. It stands out as the initial antimicrobial agent to utilize this distinct mechanism of selectivity [1].

Psammaplin A, a marine metabolite, functions as a robust inhibitor of HDAC and DNA methyltransferases, displaying notable potency and selectivity as a DAC1 inhibitor, with an IC50 value of 0.9 nM. It exhibits antimicrobial effects against Gram-positive bacteria and inhibits both DNA synthesis and DNA gyrase activity, also demonstrating antitumor activity[1][2].

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

844-TFM is an NBTI (novel bacterial topoisomerase inhibitor) DNA gyrase inhibitor (IC50: 1.5 μM). 844-TFM exhibits bactericidal activity against Mycobacterium abscessus.

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

Levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth.

Anti-MRSA agent 7 (Compound 12) serves as a potent antibacterial compound effectively inhibiting both S. aureus and E. coli DNA gyrases, as well as topo IV enzymes from the same organisms, with IC50 values of 0.185 μM, 0.365 μM, 0.341 μM, and 0.059 μM, respectively [1].

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

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

Danofloxacin (Danofloxacin free base) is a fluoroquinolone antibiotic used in veterinary medicine.

Gatifloxacin (CG5501) is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

Levofloxacin sodium is a synthetic fluoroquinolones antibacterial. It inhibits the supercoiling activity of bacterial DNA gyrase, so that halting DNA replication.

BRD7116 competitively binds to bacterial DNA gyrase, with cell-non-autonomous anti-leukemia activity.

Topoisomerase IV inhibitor 2 (compound 5d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.35 μM for TOPO IV and 0.55 μM for DNA gyrase. It also demonstrates antibacterial properties, with minimum inhibitory concentrations (MICs) of 1.985 μM against Staphylococcus aureus Newman and 0.744 μM against Escherichia coli ATCC8739 [1].

PD 163449 is a bioactive molecule of 4-pyridone group that inhibits bacterial type IIA topoisomerase (DNA gyrase and topoisomerase IV).

TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].

Nalidixic acid (NSC-82174) is a synthetic 1, 8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.

Flumequine (R-802) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.

Cyclothialidine is an inhibitor of DNA gyrase.

UIAA-II-232 (compound 19b) is a potent inhibitor of DNA gyrase catalytic (IC 50= 3.5 μM).

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).

AZD-5099 is a DNA gyrase modulator potentially for the treatment of bacterial infection.

NBTIs-IN-5 (Compound 5r) is an NBTI (novel bacterial topoisomerase inhibitor) DNA gyrase inhibitor that acts on Mycobacterium abscessus (Mabs) DNA procyclase (IC50: 1.5 μM). NBTIs-IN-5 showed inhibitory effects on the growth of Mabsbamboo bacteria (MIC90: 0.4 μM).

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).

Tryptanthrin is a natural DNA gyrase inhibitor.