To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL against , , , and , respectively. The in vivo enzyme inhibition assay displayed the most potent topoisomerase II (IC = 13.5 µg/mL) and topoisomerase IV (IC = 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound into the topoisomerase II active site to determine the probable binding conformation. In summary, compound may serve as potential topoisomerase II inhibitor.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480153PMC
http://dx.doi.org/10.3390/molecules24071311DOI Listing

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