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 Bacillus...

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Detalles Bibliográficos
Autores principales: Sun, Juan, Lv, Peng-Cheng, Yin, Yong, Yuan, Rong-Ju, Ma, Jian, Zhu, Hai-Liang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2013
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3726784/
https://www.ncbi.nlm.nih.gov/pubmed/23922790
http://dx.doi.org/10.1371/journal.pone.0069751
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author Sun, Juan
Lv, Peng-Cheng
Yin, Yong
Yuan, Rong-Ju
Ma, Jian
Zhu, Hai-Liang
author_facet Sun, Juan
Lv, Peng-Cheng
Yin, Yong
Yuan, Rong-Ju
Ma, Jian
Zhu, Hai-Liang
author_sort Sun, Juan
collection PubMed
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 IC(50) 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.
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spelling pubmed-37267842013-08-06 Synthesis, Structure and Antibacterial Activity of Potent DNA Gyrase Inhibitors: N′-Benzoyl-3-(4-Bromophenyl)-1H-Pyrazole-5-Carbohydrazide Derivatives Sun, Juan Lv, Peng-Cheng Yin, Yong Yuan, Rong-Ju Ma, Jian Zhu, Hai-Liang PLoS One Research Article 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 IC(50) 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. Public Library of Science 2013-07-29 /pmc/articles/PMC3726784/ /pubmed/23922790 http://dx.doi.org/10.1371/journal.pone.0069751 Text en © 2013 Sun et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited.
spellingShingle Research Article
Sun, Juan
Lv, Peng-Cheng
Yin, Yong
Yuan, Rong-Ju
Ma, Jian
Zhu, Hai-Liang
Synthesis, Structure and Antibacterial Activity of Potent DNA Gyrase Inhibitors: N′-Benzoyl-3-(4-Bromophenyl)-1H-Pyrazole-5-Carbohydrazide Derivatives
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
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3726784/
https://www.ncbi.nlm.nih.gov/pubmed/23922790
http://dx.doi.org/10.1371/journal.pone.0069751
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