Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives.
A total of 19 novel (3a-3s) N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide analogs were designed, synthesized, and evaluated for biological activities as potential DNA gyrase inhibitors. The results showed that compound 3k can strongly inhibit Staphylococcus aureus DNA gyrase and Bac...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2013-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC3726784?pdf=render |
| _version_ | 1819112098780676096 |
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| author | Juan Sun Peng-Cheng Lv Yong Yin Rong-Ju Yuan Jian Ma Hai-Liang Zhu |
| author_facet | Juan Sun Peng-Cheng Lv Yong Yin Rong-Ju Yuan Jian Ma Hai-Liang Zhu |
| author_sort | Juan Sun |
| collection | DOAJ |
| description | A total of 19 novel (3a-3s) N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide analogs were designed, synthesized, and evaluated for biological activities as potential DNA gyrase inhibitors. The results showed that compound 3k can strongly inhibit Staphylococcus aureus DNA gyrase and Bacillus subtilis DNA gyrase (with IC50 of 0.15 µg/mL and 0.25 µg/mL, respectively). Structure-activity relationships were also discussed base on the biological and docking simulation results. |
| first_indexed | 2024-12-22T04:08:07Z |
| format | Article |
| id | doaj.art-7e0be67b2a5643c8ad636e4e7638ec03 |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-22T04:08:07Z |
| publishDate | 2013-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-7e0be67b2a5643c8ad636e4e7638ec032022-12-21T18:39:35ZengPublic Library of Science (PLoS)PLoS ONE1932-62032013-01-0187e6975110.1371/journal.pone.0069751Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives.Juan SunPeng-Cheng LvYong YinRong-Ju YuanJian MaHai-Liang ZhuA total of 19 novel (3a-3s) N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide analogs were designed, synthesized, and evaluated for biological activities as potential DNA gyrase inhibitors. The results showed that compound 3k can strongly inhibit Staphylococcus aureus DNA gyrase and Bacillus subtilis DNA gyrase (with IC50 of 0.15 µg/mL and 0.25 µg/mL, respectively). Structure-activity relationships were also discussed base on the biological and docking simulation results.http://europepmc.org/articles/PMC3726784?pdf=render |
| spellingShingle | Juan Sun Peng-Cheng Lv Yong Yin Rong-Ju Yuan Jian Ma Hai-Liang Zhu Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. PLoS ONE |
| title | Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. |
| title_full | Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. |
| title_fullStr | Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. |
| title_full_unstemmed | Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. |
| title_short | Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives. |
| title_sort | synthesis structure and antibacterial activity of potent dna gyrase inhibitors n benzoyl 3 4 bromophenyl 1h pyrazole 5 carbohydrazide derivatives |
| url | http://europepmc.org/articles/PMC3726784?pdf=render |
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