Synthesis and Biological Evaluation of Novel Naphthoquinone-4-aminosulfonamide Derivatives as Antibacterial Agents

Objective: To address the serious challenge of antibiotic resistance, this study aimed to synthesize a series of novel naphthoquinone-4-aminosulfonamide derivatives and evaluate their anti-Helicobacter pylori (H. pylori) activity. Methods: The target derivatives were synthesized using benzenesulfonyl chlorides, N-Boc-1,4-butanediamine, and 2-chloro-1,4-naphthoquinone as starting materials. All synthesized compounds were characterized by HRMS and NMR spectroscopy. Antibacterial activity was assessed using the broth microdilution method. Results and Discussion: Nine target compounds were successfully synthesized. All compounds exhibited significant inhibitory activity against H. pylori, with minimum inhibitory concentration (MIC) values ranging from 4 to 16 μg/mL. Conclusions: These results indicate the potential of the synthesized derivatives as promising candidates for novel anti-H. pylori therapies.