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*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

19 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)244-254
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume48
DOIs
StatePublished - 02 2012
Externally publishedYes

Keywords

  • 2-Fluorophenyl-5-methyl-1-(3,4,5- trimethoxybenzyl)benzimidazole
  • Antibiotic resistant
  • Benzimidazole
  • Helicobacter pylori
  • Human gastric epithelial cells
  • Interleukin-8

Fingerprint

Dive into the research topics of 'Synthesis and bioevaluation of novel 3,4,5-trimethoxybenzylbenzimidazole derivatives that inhibit Helicobacter pylori-induced pathogenesis in human gastric epithelial cells'. Together they form a unique fingerprint.

Cite this