DNA gyrase Inhibitor

Topoisomerase IN-7 is a bacterial topoisomerase inhibitor, with an IC₅₀ value of 47 nM against Staphylococcus aureus DNA gyrase, 85 nM against Escherichia coli DNA gyrase, and 1 nM against Escherichia coli topoisomerase IV. Topoisomerase IN-7 inhibits the supercoiling activity of DNA gyrase, suppresses the relaxation activity of topoisomerase IV, stabilizes single-stranded DNA cleavage complexes, inhibits biofilm formation of specific bacteria, stimulates biofilm formation of methicillin-resistant Staphylococcus aureus, and exhibits bactericidal activity. Topoisomerase IN-7 is selective for bacterial topoisomerases over human topoisomerase IIα, shows moderate cytotoxicity, and inhibits the hERG potassium channel. Topoisomerase IN-7 can be used in studies of bacterial infections.

GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.

Abimufloxacin (OPS-2071) is a broad-spectrum quinolone antibacterial agent. Abimufloxacin inhibits the supercoiling activity of DNA gyrase, the decatenation activity of topoisomerase IV, the activation and proliferation of T cells, macrophage activity, as well as the production of TNF-α and IFN-γ. Abimufloxacin exhibits activity against enteropathogenic Gram-positive bacteria, Gram-negative bacteria, quinolone-resistant bacteria, and Crohn's disease-associated bacteria (including Clostridioides difficile and Campylobacter jejuni). Abimufloxacin alleviates colonic inflammation in a mouse model of T cell-mediated colitis. Abimufloxacin can be used in research related to diseases such as intestinal infections and Crohn's disease.

Antibacterial agent 372 is a potent antibacterial agent. Antibacterial agent 372 is a DNA gyrase inhibitor that binds to the ATP-binding pocket of the GyrB subunit, downregulates gyrB gene expression, and impedes DNA replication and supercoiling. Antibacterial agent 372 exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria. Antibacterial agent 372 can be used for research on microbial infections.

Topoisomerase II-IN-26 is a dual bacterial type II topoisomerase (Top II) inhibitor, with IC₅₀ values of 0.081 μM and 0.093 μM against Staphylococcus aureus DNA gyrase and topoisomerase IV, respectively, and IC₅₀ values of 0.906 μM and 0.103 μM against Escherichia coli DNA gyrase and topoisomerase IV, respectively. Topoisomerase II-IN-26 also shows high selectivity for human topoisomerase IIα. Topoisomerase II-IN-26 inhibits biofilm formation, reduces the metabolic activity of mature biofilms, exhibits activity against Staphylococcus aureus, MRSA strains, Escherichia coli and Acinetobacter baumannii, and possesses a post-antibiotic effect. Topoisomerase II-IN-26 can be used for the research of bacterial infections such as Staphylococcus aureus and MRSA.

Antibacterial agent 352 is an orally active Antibacterial agent. Antibacterial agent 352 binds to the active cavity of Staphylococcus aureus DNA gyrase via hydrogen bonding, π-π stacking and hydrophobic interactions, thereby blocking bacterial DNA synthesis. Antibacterial agent 352 exhibits antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus pumilus, Staphylococcus epidermidis and Enterococcus faecalis. Antibacterial agent 352 can disrupt established Staphylococcus aureus biofilms and inhibit the formation of Staphylococcus aureus biofilms. Antibacterial agent 352 can be used in the research of Staphylococcus aureus wound infections.

Albicidin is a peptide antibiotic with phytotoxic activity. Albicidin potently inhibits bacterial and plant DNA gyrase at nanomolar concentrations, blocks DNA replication, and exhibits excellent antibacterial efficacy against multidrug-resistant bacteria. Albicidin possesses bactericidal activity against Gram-positive and Gram-negative microorganisms, and acts as a virulence factor for the systemic plant infection by Xanthomonas albilineans. Albicidin can be used in studies related to bacterial infections and sugarcane leaf blight.

Topoisomerase IV-IN-3 is a Staphylococcus aureus Topoisomerase IV inhibitor, DNA gyrase inhibitor and antibacterial agent. Topoisomerase IV-IN-3 has IC₅₀ values of 1.32 μM and 0.48 μM against topoisomerase IV, and 0.88 μM and 0.54 μM against DNA gyrase. Topoisomerase IV-IN-3 inhibits decatenation, ATPase, and supercoiling activities of its target enzymes. Topoisomerase IV-IN-3 exerts antibacterial activity against Gram-positive and Gram-negative bacterial strains. Topoisomerase IV-IN-3 exhibits low cytotoxicity toward human fibroblast cells. Topoisomerase IV-IN-3 can be used for the research of bacterial infections.