Synthesis and Biological Evaluation of New Nitroimidazole Derivatives as Anti-Helicobacter pylori Agents Against Metronidazole-Resistant Strains

合成新型硝基咪唑衍生物并对其作为抗幽门螺杆菌药物对抗甲硝唑耐药菌株的生物学性能进行评价

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Abstract

Since several Helicobacter pylori strains have become resistant to metronidazole, new nitroimidazole derivatives based on metronidazole were designed and synthesized with different substituents on imidazole nitrogen. The activity of the synthesized compounds was evaluated against 20 clinically isolated metronidazole-resistant H. pylori strains. Some synthesized compounds were effective against those metronidazole-resistant H. pylori strains. Three compounds exhibited the most potent inhibitory activities (MIC(50) = 8 µg/mL and MIC(90) = 16 µg/mL).

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