Synthesis of benzimidazole derivatives as potent β-glucuronidase inhibitors

Muhammad Taha, Nor Hadiani Ismail, Syahrul Imran, Manikandan Selvaraj, Hesham Rashwan, Fatin Ummi Farhanah, Fazal Rahim, Krishnan Selvarajan Kesavanarayanan, Muhammad Ali

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42 Citations (Scopus)


Twenty five 4, 6-dichlorobenzimidazole derivatives (1-25) have been synthesized and evaluated against β-glucuronidase inhibitory activity. The compounds which actively inhibit β-glucuronidase activity have IC50 values ranging between 4.48 and 46.12 μM and showing better than standard d-saccharic acid 1,4 lactone (IC50 = 48.4 ± 1.25 μM). Molecular docking provided potential clues to identify interactions between the active molecules and the enzyme which further led us to identify plausible binding mode of all the benzimidazole derivatives. This study confirmed that presence of hydrophilic moieties is crucial to inhibit the human β-glucuronidase.

Original languageEnglish
Pages (from-to)36-44
Number of pages9
JournalBioorganic Chemistry
Publication statusPublished - 12 Jun 2015
Externally publishedYes


  • Benzimidazole
  • Docking studies
  • Synthesis
  • β-Glucuronidase

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