Topoisomerase IN-7

Topoisomerase IN-7 (compound 13) displays potent broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacterial strains, with MIC values as low as 0.008 μg/mL^[1].
Topoisomerase IN-7 (1-10 μM) potently inhibits bacterial DNA gyrase and TopoIV with low nanomolar IC₅₀ values, while showing minimal inhibition of human topoisomerase IIα, demonstrating high target selectivity^[1].
Topoisomerase IN-7 dose-dependently inhibits biofilm formation in Acinetobacter baumannii and Escherichia coli, with 80% and >92% inhibition at 1/2 MIC respectively, but slightly inhibits or stimulates biofilm formation in MRSA depending on concentration^[1].
Topoisomerase IN-7 (24 h) induces a postantibiotic effect in Acinetobacter baumannii at 1× and 8× MIC, in Escherichia coli at 8× MIC, but not in MRSA at tested concentrations^[1].
Topoisomerase IN-7 (2 μM; 1 h) has moderate aqueous solubility and medium metabolic stability in mouse liver microsomes, but exhibits high lipophilicity and high plasma protein binding, indicating a need for pharmacokinetic optimization^[1].
Topoisomerase IN-7 inhibits hERG potassium channels with an IC₅₀ of 5.36 μM, showing improved hERG selectivity relative to earlier NBTIs^[1].
Topoisomerase IN-7 (24 h) exhibits dose-dependent bactericidal activity against Acinetobacter baumannii, Escherichia coli, and MRSA, with no bacterial regrowth after 24 h at 8× MIC^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.