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Herein, we have synthesized a series of novel fifteen 2-aryl benzimidazole derivatives  8a–o  and tested their bioactivity as potent urease inhibitors. The structures of the  8a–o  were elucidated using spectroscopic technics ( 1 H-NMR,  13 C-NMR, MS), elemental analysis, and melting point. The urease inhibition activity was evaluated using the urease enzyme inhibition kit. All  8a–o  showed higher urease inhibition activity (7.74 to 21.18 µM) in comparison to thiourea and hydroxyurea as standard (IC 50 : 22 and 100 µM respectively).  8m ,  8n , and  8o  exhibited the best activity with the IC 50  value of 7.74, 8.09, and 8.56 µM respectively. Docking study represented the possible mode of interactions between the most active compound and the residues of the enzyme’s active site. To investigate the cytotoxicity profile of the target compounds, the MTT assay was performed on two different cell lines. The results showed that all  8a–o  derivatives display IC50 values higher than 50 µM toward both tested cell lines.

2-Aryl Benzimidazole Derivatives Act as Potent Urease Inhibitors; Synthesis, Bioactivity and Molecular Docking Study