Synthesis of β-Ketosulfone Derivatives As New Non-Cytotoxic Urease Inhibitors In Vitro

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Author(s): Sarosh Iqbal*, Ajmal Khan, Rashid Nazir, Shumaila Kiran, Shahnaz Perveen, Khalid Mohammed Khan*, M. Iqbal Choudhary*.

Journal Name: Medicinal Chemistry

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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.

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

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Article Details

(E-pub Abstract Ahead of Print)
DOI: 10.2174/1573406415666190415163309
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