2-(2'-Pyridyl) Benzimidazole Analogs and their β-Glucuronidase Inhibitory Activity.

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