Synthesis and β-Glucuronidase Inhibitory Potential of Benzimidazole Derivatives

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-glucuronidase inhibitors. A structure-activity relationship has also been studied.