topoisomerase iv

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.

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 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].

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).

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.

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.

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.

Anti bacterial agent 236 (Compound 4l), an orally effective inhibitor of DNA gyrase and topoisomerase IV (with IC50 values of 3.2 and 300 nM in Staphylococcus aureus, respectively), exhibits broad-spectrum antibacterial activity. It also demonstrates favorable pharmacokinetic properties in mice.

BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. The minimum inhibitory concentration (MIC90) of BWC0977 against MDR (multi-drug resistant) Gram-negative bacteria ranges from 0.03 to 2 µg mL.

Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.

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.