Abstract

Background: Peptic ulcer and urolithiasis are largely due to infection caused by ureaseproducing 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 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-ketosulfones as novel and non-cytotoxic urease inhibitors.

Keywords: Urease inhibitors, β-ketosulfones, peptic ulcer, urolithiasis, non-cytotoxic, H. pylori.