Background: Peptic ulcer and urolithiasis are largely due to infection caused by urease producing bacteria. Therefore, discovery of urease inhibitors is an important area of medicinal chemistry research.
Objective: The main goal of the work was to identify novel urease inhibitors with no cytotoxicity. Method: During the current study, a series of β-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential. Results: Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 µM, in comparison to standard thiourea (IC50 = 21 ± 0.11 µM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line. Conclusion: This study has identified β-keto-sulfones as novel and non-cytotoxic urease inhibitors.