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Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents
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| Zeitschriftentitel: | Molecules |
|---|---|
| Personen und Körperschaften: | , , , , , , , , |
| In: | Molecules, 24, 2019, 7, S. 1311 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
MDPI AG
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| Schlagwörter: |
| author_facet |
Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai |
|---|---|
| author |
Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai |
| spellingShingle |
Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai Molecules Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science |
| author_sort |
chu, ming-jie |
| spelling |
Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai 1420-3049 MDPI AG Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science http://dx.doi.org/10.3390/molecules24071311 <jats:p>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.</jats:p> Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents Molecules |
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10.3390/molecules24071311 |
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MDPI AG, 2019 |
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| title |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_unstemmed |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_full |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_fullStr |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_full_unstemmed |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_short |
Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_sort |
discovery of novel triazole-containing pyrazole ester derivatives as potential antibacterial agents |
| topic |
Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science |
| url |
http://dx.doi.org/10.3390/molecules24071311 |
| publishDate |
2019 |
| physical |
1311 |
| description |
<jats:p>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.</jats:p> |
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| author | Chu, Ming-Jie, Wang, Wei, Ren, Zi-Li, Liu, Hao, Cheng, Xiang, Mo, Kai, Wang, Li, Tang, Feng, Lv, Xian-Hai |
| author_facet | Chu, Ming-Jie, Wang, Wei, Ren, Zi-Li, Liu, Hao, Cheng, Xiang, Mo, Kai, Wang, Li, Tang, Feng, Lv, Xian-Hai, Chu, Ming-Jie, Wang, Wei, Ren, Zi-Li, Liu, Hao, Cheng, Xiang, Mo, Kai, Wang, Li, Tang, Feng, Lv, Xian-Hai |
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| description | <jats:p>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.</jats:p> |
| doi_str_mv | 10.3390/molecules24071311 |
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| spelling | Chu, Ming-Jie Wang, Wei Ren, Zi-Li Liu, Hao Cheng, Xiang Mo, Kai Wang, Li Tang, Feng Lv, Xian-Hai 1420-3049 MDPI AG Chemistry (miscellaneous) Analytical Chemistry Organic Chemistry Physical and Theoretical Chemistry Molecular Medicine Drug Discovery Pharmaceutical Science http://dx.doi.org/10.3390/molecules24071311 <jats:p>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.</jats:p> Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents Molecules |
| spellingShingle | Chu, Ming-Jie, Wang, Wei, Ren, Zi-Li, Liu, Hao, Cheng, Xiang, Mo, Kai, Wang, Li, Tang, Feng, Lv, Xian-Hai, Molecules, Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents, Chemistry (miscellaneous), Analytical Chemistry, Organic Chemistry, Physical and Theoretical Chemistry, Molecular Medicine, Drug Discovery, Pharmaceutical Science |
| title | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_full | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_fullStr | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_full_unstemmed | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_short | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| title_sort | discovery of novel triazole-containing pyrazole ester derivatives as potential antibacterial agents |
| title_unstemmed | Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents |
| topic | Chemistry (miscellaneous), Analytical Chemistry, Organic Chemistry, Physical and Theoretical Chemistry, Molecular Medicine, Drug Discovery, Pharmaceutical Science |
| url | http://dx.doi.org/10.3390/molecules24071311 |