Synthesis of benzimidazole derivatives as potent β-glucuronidase inhibitors

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