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Title: Discovery of novel triazole-containing pyrazole ester derivatives as potential antibacterial agents
Authors: Chu, Ming-Jie
Liu, Hao
Cheng, Xiang
Mo, Kai
Wang, Li
Tang, Feng
Lv, Xian-Hai
Wang, Wei
Ren, Zi-Li
Keywords: Pyrazole
Issue Date: 2019
Source: Chu, M.-J., Wang, W., Ren, Z.-L., Liu, H., Cheng, X., Mo, K., . . . Lv, X.-H. (2019). Discovery of novel triazole-containing pyrazole ester derivatives as potential antibacterial agents. Molecules, 24(7), 1311-. doi:10.3390/molecules24071311
Series/Report no.: Molecules
Abstract: 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 4d 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 Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 µg/mL) and topoisomerase IV (IC50 = 24.2 µg/mL) inhibitory activity. Molecular docking was performed to position compound 4d into the topoisomerase II active site to determine the probable binding conformation. In summary, compound 4d may serve as potential topoisomerase II inhibitor.
ISSN: 1420-3049
DOI: 10.3390/molecules24071311
Rights: © 2019 The Authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SPMS Journal Articles

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