Abstract
Synthesis of 2-(2'-pyridyl) benzimidazole analogs 1-11 have been carried out and evaluated for in vitro beta-glucuronidase inhibitory potential. The compounds 4 (IC50 = 4.06 +/- 0.34 mu M), 5 (IC50 = 09.63 +/- 0.81 mu M), 1 (IC50 = 19.66 +/- 0.44 mu M), 7 (IC50 = 24.75 +/- 0.25 mu M), 6 (IC50 = 26.30 +/- 1.37 mu M), and 3 (IC50 = 32.11 +/- 0.89 mu M), showed beta-glucuronidase inhibitory activity superior to the standard D-saccharic acid 1,4-lactone, with (IC50 = 48.4 +/- 1.25 mu M). Based on structure-activity relationship, we discover a new class of potent beta-glucuronidase inhibitors.