Benzimidazole derivatives 1-24 have been synthesized and their in vitro β-glucuronidase inhibitory activitiy was evaluated. Compounds 15 (IC50= 6.33±0.40 μM), 7 (IC50= 22.0±0.33 μM), 2 (IC50= 23.1±1.78 μM), 17 (IC50= 23.9±1.46 μM), and 3 (IC50= 33.8±1.61 μM) showed more potent β-glucuronidase inhibitory activity than the standard (D-saccharic acid 1, 4 lactone, IC50= 48.4±1.25 μM). This study has identified a new series of potential β- ...