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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.

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