2-Aryl Benzimidazole Derivatives Act as Potent Urease Inhibitors; Synthesis, Bioactivity and Molecular Docking Study

Ebrahim Saeedian Moghadam, Abdullah Mohammed Al-Sadi, Meysam Talebi, Massoud Amanlou, Mohsen Amini, Raid Abdel-Jalil*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


Herein, we have synthesized a series of novel fifteen 2-aryl benzimidazole derivatives 8a–o and tested their bioactivity as potent urease inhibitors. The structures of the 8a–o were elucidated using spectroscopic technics (1H-NMR, 13C-NMR, MS), elemental analysis, and melting point. The urease inhibition activity was evaluated using the urease enzyme inhibition kit. All 8a–o showed higher urease inhibition activity (7.74 to 21.18 µM) in comparison to thiourea and hydroxyurea as standard (IC50: 22 and 100 µM respectively). 8m, 8n, and 8o exhibited the best activity with the IC50 value of 7.74, 8.09, and 8.56 µM respectively. Docking study represented the possible mode of interactions between the most active compound and the residues of the enzyme’s active site. To investigate the cytotoxicity profile of the target compounds, the MTT assay was performed on two different cell lines. The results showed that all 8a–o derivatives display IC50 values higher than 50 µM toward both tested cell lines.

Original languageEnglish
JournalPolycyclic Aromatic Compounds
Publication statusAccepted/In press - 2021
Externally publishedYes


  • Benzimidazole
  • heterocyclic chemistry
  • MTT
  • synthesis
  • urease inhibitor

ASJC Scopus subject areas

  • Organic Chemistry
  • Polymers and Plastics
  • Materials Chemistry

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