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首页> 外文期刊>Journal of infection and chemotherapy: official journal of the Japan Society of Chemotherapy >Potent antibacterial activity of Y-754, a novel benzimidazole compound with selective action against Helicobacter pylori.
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Potent antibacterial activity of Y-754, a novel benzimidazole compound with selective action against Helicobacter pylori.

机译:Y-754的强效抗菌活性,一种新型的苯并咪唑化合物,对幽门螺杆菌具有选择性。

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摘要

Y-754, a novel benzimidazole compound, was investigated for in vitro and in vivo antibacterial activity. Unlike amoxicillin, clarithromycin, and metronidazole, the compound had no activity against common aerobic and anaerobic bacteria other than Helicobacter pylori. The minimum inhibitory concentration of Y-754 against H. pylori, at 0.025 microg/ml, was nearly equal to that of amoxicillin and clarithromycin. The respective concentrations of Y-754, amoxicillin, clarithromycin, and metronidazole required to inhibit 90% of 39 isolates of H. pylori were 0.05, 0.39, 6.25, and 25 microg/ml, indicating the potent activity of Y-754, including activity against clarithromycin- and metronidazole-resistant strains. The anti-H. pylori activity of Y-754 was potent even at pH 5.5 and was bactericidal at concentrations of 0.1 microg/ml and above. Exposure of H. pylori to Y-754 did not result in the induction of drug-resistant mutation. Oral administration (10 mg/kg twice a day for 7 days) to Mongolian gerbils infectedwith strain ATCC 43504 demonstrated that Y-754 was effective in H. pylori eradication and that its eradication efficacy increased in line with the progress of damage to the gastric mucosa caused by H. pylori infection. Y-754 was also efficacious in the treatment of infection by the clarithromycin-resistant strain OIT-36. The results obtained lead to the expectation that the new benzimidazole Y-754 will, in the near future, be used for H. pylori eradication therapy in peptic ulcer patients.
机译:研究了新型苯并咪唑化合物Y-754的体外和体内抗菌活性。与阿莫西林,克拉霉素和甲硝唑不同,该化合物对除幽门螺杆菌外的常见需氧和厌氧细菌没有活性。 Y-754对幽门螺杆菌的最低抑菌浓度为0.025微克/毫升,几乎等于阿莫西林和克拉霉素的抑菌浓度。抑制39株幽门螺杆菌的90%所需的Y-754,阿莫西林,克拉霉素,甲硝唑的各自浓度分别为0.05、0.39、6.25和25 microg / ml,表明Y-754的有效活性包括活性对抗克拉霉素和甲硝唑耐药菌株。反H。 Y-754的幽门螺杆菌活性即使在pH 5.5下也有效,并且在0.1μg/ ml及以上的浓度下具有杀菌作用。幽门螺杆菌暴露于Y-754不会导致耐药突变的诱导。对感染ATCC 43504菌株的蒙古沙鼠口服给药(每天两次,每次10 mg / kg,共7天)表明,Y-754在根除幽门螺杆菌方面有效,并且根除对胃黏膜的损害程度提高了根除功效由幽门螺杆菌感染引起。 Y-754在抵抗克拉霉素抗性菌株OIT-36的感染中也有效。获得的结果导致期望新的苯并咪唑Y-754将在不久的将来用于消化性溃疡患者的幽门螺杆菌根除疗法。

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