topoisomerase-iv

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].

Topoisomerase IV inhibitor 2 (compound 7d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.23 μM for TOPO IV and 0.43 μM for DNA gyrase. It demonstrates antibacterial efficacy, with minimum inhibitory concentrations (MICs) of 0.972 μM against Staphylococcus aureus Newman and 0.608 μM against Escherichia coli ATCC8739 [1].

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.

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

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.

Prulifloxacin (NM441) is a broad-spectrum fluoroquinolone antibiotic. It Inhibits bacterial DNA synthesis by inhibiting the activity of bacterial DNA topoisomerase II and IV.

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.

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).

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

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.

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

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.

NBTIs-IN-4 is able to act on a wide range of Gram-positive pathogens with significant antibacterial effects, exhibiting inhibition of DNA rotamases and topoisomerase IV with low resistance rates.

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].

Levofloxacin-d8 is a deuterated compound of Levofloxacin. Levofloxacin has a CAS number of 100986-85-4. Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

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].

Gatifloxacin (mesylate) is an antibiotic of the fourth-generation fluoroquinolone family. It also inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts superhelical activity (IC50: 875 μM) and exhibits antibacterial activity against Pseudomonas aeruginosa E. coli with MIC values of 10-80 μM, without affecting the closely related enzyme topoisomerase IV.

Gemifloxacin mesylate (Gemifloxacin mesylate) inhibits activities of DNA gyrase and topoisomerase IV, thereby inhibiting DNA replication and eventually bacterial growth. Gemifloxacin Mesylate is the mesylate salt form of gemifloxacin, a synthetic broad-spectrum fluoroquinolone with antibacterial activity. This fluoroquinolone exerts an enhanced spectrum of activity against gram-positive bacteria such as Streptococcus pneumonia and Staphylococcus aureus, in addition to its activity against gram-negative bacteria.

Levofloxacin-d3 is a deuterated compound of Levofloxacin. Levofloxacin has a CAS number of 100986-85-4. Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

CBR-2092 is a DNA-directed RNA polymerase and DNA topoisomerase inhibitor. CBR-2092 exhibited rifampin-like potency as an inhibitor of RNA polymerase, was an equipotent (balanced) inhibitor of DNA gyrase and DNA topoisomerase IV, and retained activity against a prevalent quinolone-resistant variant. Studies of mutant strains that exhibited reduced susceptibility to CBR-2092 further substantiated RNA polymerase as the primary cellular target of CBR-2092, with DNA gyrase and DNA topoisomerase IV being secondary and tertiary targets, respectively, in strains exhibiting preexisting rifampin resistance.

Type II topoisomerase inhibitor 1 is a potent and selective inhibitor of E. coli DNA gyrase with an IC50 value of 1.7 nM and forms hydrogen bonds with the Asp73 residue. It inhibits topoisomerase IV activity with an IC50 value of 0.98 μM and is applicable in the antibacterial area [1] [2].

Gatifloxacin sesquihydrate, a bacterial DNA gyrase inhibitor, is used to treat tuberculosis and pneumonia.