dna-gyrase

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-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-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase DNA Gyrase, exhibiting 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 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-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 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-8 is a potent DNA gyrase inhibitor, exhibiting 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 and DNA Gyrase, exhibiting significant 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.

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.

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 effective against both Gram-positive and Gram-negative bacteria. It operates by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, enzymes crucial for separating bacterial DNA, thereby preventing cell division.

Tryptanthrin is a natural DNA gyrase inhibitor.

Nalidixic acid sodium salt (Baktogram) is an antimicrobial agent with a limited bacteriocidal spectrum.

Ciprofloxacin (Bay-09867), a synthetic broad spectrum fluoroquinolone antibiotic, inhibits bacterial DNA gyrase. It is more active against Gram-negative bacteria than Gram-positive bacteria.

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

Gatifloxacin hydrochloride (AM-1155 hydrochloride) is a fourth-generation fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV.

Levofloxacin hydrate (Cravit hydrate) 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.

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

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.

Sparfloxacin (CI-978) is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase, thus preventing DNA replication and transcription.

Balofloxacin, a quinolone antibiotic, can inhibit the synthesis of bacterial DNA by interfering with the DNA gyrase.

Danofloxacin mesylate (CP 76136-27) is a synthetic antibacterial agent of the fluoroquinolone class that primarily inhibits bacterial DNA-gyrase.

Lomefloxacin hydrochloride (Okacyn) inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to a decrease in DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis. Lomefloxacin Hydrochloride is the hydrochloride salt form of lomefloxacin, a synthetic broad-spectrum fluoroquinolone with antibacterial activity.

Levofloxacin ((-)-Ofloxacin) is a synthetic fluoroquinolone antibiotic that inhibits the superhelical activity of bacterial DNA rotamase and prevents DNA replication. Levofloxacin is a broad-spectrum antibiotic used for the treatment of a wide range of bacterial infections.

Fleroxacin (RO 23-6240) is a broad-spectrum antimicrobial fluoroquinolone that strongly inhibits the DNA-supercoiling activity of DNA gyrase.

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

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.

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

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).

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

Anti-MRSA agent 7 (Compound 12) is a potent antibacterial compound that effectively inhibits 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 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.

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

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.

Ofloxacin-d8 is a deuterated compound of Ofloxacin. Ofloxacin has a CAS number of 82419-36-1. Ofloxacin 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.

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

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

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 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].