Synthesis, Structure and Antibacterial Activity of Potent DNA Gyrase Inhibitors: N′-Benzoyl-3-(4-Bromophenyl)-1H-Pyrazole-5-Carbohydrazide Derivatives

被引：18

作者：

Sun, Juan ^{[1
]}

Lv, Peng-Cheng ^{[1
]}

Yin, Yong ^{[1
]}

Yuan, Rong-Ju ^{[2
]}

Ma, Jian ^{[2
]}

Zhu, Hai-Liang ^{[1
,2
]}

机构：

[1] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210008, Jiangsu, Peoples R China

[2] Shandong Univ Technol, Sch Life Sci, Zibo, Peoples R China

来源：

PLOS ONE | 2013年 / 8卷 / 07期

关键词：

STAPHYLOCOCCUS-AUREUS; BIOLOGICAL EVALUATION; PYRAZOLE DERIVATIVES; ANTIMICROBIAL AGENTS; DESIGN; TOPOISOMERASES; ANALOGS;

D O I：

10.1371/journal.pone.0069751

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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 mu g/mL and 0.25 mu g/mL, respectively). Structure-activity relationships were also discussed base on the biological and docking simulation results.

引用

页数：9

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