topoisomerase-iv

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

Trovafloxacin mesylate is a fluoroquinolone antibiotic and a dual inhibitor of DNA gyrase and topoisomerase IV, as well as a selective inhibitor of the Pannexin 1 channel (IC50 = 4 μM). With oral bioactivity and cell permeability, Trovafloxacin does not inhibit connexin 43 or PANX2, and is used for antibacterial therapy.

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.

TopoisomeraseIV-IN-3 is an inhibitor of Staphylococcus aureus topoisomerase IV (TopoisomeraseIV), a DNA gyrase inhibitor, and an antimicrobial agent. It has IC50 values of 1.32 μM and 0.48 μM for topoisomerase IV, and 0.88 μM and 0.54 μM for DNA gyrase. TopoisomeraseIV-IN-3 effectively inhibits the decatenation, ATPase, and supercoiling activities of its target enzymes. It demonstrates antibacterial activity against both Gram-positive and Gram-negative strains while exhibiting low cytotoxicity to human fibroblasts. This compound is applicable for research related to bacterial infections.

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].

Topoisomerase IV inhibitor 2 (compound 5d) is an effective Topo IV inhibitor with IC50 values of 0.35 μM and 0.55 μM for Topo IV and DNA cyclase, respectively, and has antibacterial activity.

Topoisomerase IV, E. coli (EC 5.99.1.) is produced by overexpressing the parC and parE subunits in Escherichia coli. In its active form, Topoisomerase IV dissolves in a diluted buffer solution as a heterotetrameric complex.

Topoisomerase IV, Pseudomonas aeruginosa (EC 5.99.1), is prepared by overexpressing its subunits in Escherichia coli. The enzyme is soluble in a diluted buffer as a heterotetrameric complex.

Topoisomerase IV, Streptococcus pneumoniae (EC 5.99.1.), is produced by overexpressing its subunit in Escherichia coli.

Topoisomerase IV, Acinetobacter baumannii (EC 5.99.1.), is produced by overexpressing its subunits in Escherichia coli. It is dissolved in a dilute buffer solution as a heterotetrameric complex.

TopoisomeraseIV, Staphylococcus aureus (EC 5.99.1.), is produced by overexpressing the subunits in Escherichia coli.

Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) is a broad-spectrum antimicrobial carboxyfluoroquinoline.

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.

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.

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 (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 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.

Ciprofloxacin (Bay-09867) mainly targets bacterial DNA Gyrase (IC50=0.22-0.31 µM) and topoisomerase IV (IC50=0.3-1.9 µM). Ciprofloxacin is a highly active fluoroquinolone antibiotic.

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

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.

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

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.