topo iv

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

Moxifloxacin hydrochloride (BAY12-8039 HCl) is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria as well as atypical pathogens. Moxifloxacin has been linked to mild ALT elevations during therapy and to rare instances of idiosyncratic acute liver injury with symptoms and jaundice.

Pefloxacin Mesylate (Pefloxacinium mesylate) is a synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.

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.

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

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.

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

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.

Marbofloxacin (Zeniquin) is an effective, broad-spectrum antibiotic of bacterial, which inhibits DNA replication.

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.

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.

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.

Lomefloxacin (SC47111A) is a synthetic broad-spectrum fluoroquinolone with antibacterial 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.

DNA gyrase/Topo IV-IN-2 (Compound AK19) is an antibacterial agent with IC50 values of 0.783 μM and 7.136 μM for inhibiting E. coli DNA gyrase and topoisomerase IV, respectively. It exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative pathogens and inhibits biofilm formation in B. subtilis and MRSA, with a MIC of 1.9 μM. DNA gyrase/Topo IV-IN-2 is useful for researching drugs targeting resistant bacteria.

Antibacterialagent 229 (compound 8a) is a potent antimicrobial agent with antibacterial and antifungal properties. It disrupts bacterial membrane integrity and inserts into DNA. Additionally, Antibacterialagent 229 inhibits topoisomerase IV (topoisomeraseIV) activity, exhibiting an IC50 value of 10.88 µM.

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].

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].

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 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.