Abstract
Background: Peptic ulcer and urolithiasis are largely due to infection caused by urease-producing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research.
Objective: The main aim of the work was to identify novel urease inhibitors with no cytotoxicity.
Methods: During the current study, a series of beta-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 mu M, in comparison to standard thiourea (IC50 = 21 +/- 0.11 mu M). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line.
Conclusion: This study has identified beta-ketosulfones as novel and non-cytotoxic urease inhibitors.