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

Research output: Contribution to journalArticle

9 Citations (Scopus)

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)244-252
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume48
DOIs
Publication statusPublished - Feb 2012

Fingerprint

Helicobacter pylori
Stomach
Epithelial Cells
Derivatives
Adhesion
Anti-Bacterial Agents
Helicobacter Infections
Pylorus
Gastritis
Microbial Drug Resistance
Growth
Peptic Ulcer
benzimidazole
Neoplasms

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Synthesis and bioevaluation of novel 3,4,5-trimethoxybenzylbenzimidazole derivatives that inhibit Helicobacter pylori-induced pathogenesis in human gastric epithelial cells. / Chang, Chih Shiang; Liu, Ju Fang; Lin, Hwai Jeng; Lin, Chia Der; Tang, Chih Hsin; Lu, Dah Yuu; Sing, Yu Ting; Chen, Li Yu; Kao, Min Chuan; Kuo, Sheng Chu; Lai, Chih Ho.

In: European Journal of Medicinal Chemistry, Vol. 48, 02.2012, p. 244-252.

Research output: Contribution to journalArticle

Chang, Chih Shiang ; Liu, Ju Fang ; Lin, Hwai Jeng ; Lin, Chia Der ; Tang, Chih Hsin ; Lu, Dah Yuu ; Sing, Yu Ting ; Chen, Li Yu ; Kao, Min Chuan ; Kuo, Sheng Chu ; Lai, Chih Ho. / Synthesis and bioevaluation of novel 3,4,5-trimethoxybenzylbenzimidazole derivatives that inhibit Helicobacter pylori-induced pathogenesis in human gastric epithelial cells. In: European Journal of Medicinal Chemistry. 2012 ; Vol. 48. pp. 244-252.
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