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Medicinal Chemistry

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ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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Research Article

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

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

Volume 16, Issue 2, 2020

Page: [244 - 255] Pages: 12

DOI: 10.2174/1573406415666190415163309

Price: $65

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.

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