Synthesis ofβ-Ketosulfone Derivatives As New Non-Cytotoxic Urease InhibitorsIn Vitro

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.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-ketosulfones as novel and non-cytotoxic urease inhibitors.