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

Juan Sun | Zendy; PengCheng Lv | Zendy; Yong Yin | Zendy; Rong-Ju Yuan | Zendy; Jian Ma | Zendy; HaiLiang Zhu | Zendy

Open Access

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

Author(s) -

Juan Sun,

PengCheng Lv,

Yong Yin,

Rong-Ju Yuan,

Jian Ma,

HaiLiang Zhu

Publication year - 2013

Publication title -

plos one

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.99

H-Index - 332

ISSN - 1932-6203

DOI - 10.1371/journal.pone.0069751

Subject(s) - dna gyrase , carbohydrazide , chemistry , pyrazole , bacillus subtilis , antibacterial activity , docking (animal) , dna , staphylococcus aureus , stereochemistry , combinatorial chemistry , biochemistry , biology , medicinal chemistry , escherichia coli , bacteria , medicine , veterinary medicine , gene , genetics

A total of 19 novel ( 3a–3s ) N′-benzoyl-3-(4-bromophenyl)-1 H -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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