Synthesis and bioevaluation of novel 3,4,5-trimethoxybenzylbenzimidazole derivatives that inhibit Helicobacter pylori-induced pathogenesis in human gastric epithelial cells

Chih Shiang Chang, Ju Fang Liu, Hwai Jeng Lin, Chia Der Lin, Chih Hsin Tang, Dah Yuu Lu, Yu Ting Sing, Li Yu Chen, Min Chuan Kao, Sheng Chu Kuo, Chih Ho Lai

研究成果: 雜誌貢獻文章同行評審

10 引文 斯高帕斯(Scopus)

摘要

Helicobacter pylori infection is associated with gastritis, peptic ulcer, and even gastric malignancy. H. pylori's antibiotic resistance is the major obstacle preventing its eradication. A series of 3,4,5- trimethoxybenzylbenzimidazole derivatives were synthesized and evaluated for their anti-H. pylori activity. The compound, 2-fluorophenyl-5-methyl-1-(3,4,5- trimethoxybenzyl)benzimidazole (FMTMB), was determined as the most potent in the inhibition of H. pylori growth and pathogenesis of host cells. An in vitro H. pylori infection model revealed that FMTMB inhibited H. pylori adhesion and invasion of gastric epithelial cells. Results from this study provide evidence that FMTMB is a potent therapeutic agent that exhibits both anti-H. pylori growth properties and anti-H. pylori-induced pathogenesis of cells.

原文英語
頁(從 - 到)244-252
頁數9
期刊European Journal of Medicinal Chemistry
48
DOIs
出版狀態已發佈 - 二月 2012

ASJC Scopus subject areas

  • 藥物發現
  • 有機化學
  • 藥理

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