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

[ Vol. 16 , Issue. 2 ]

Author(s):

Sarosh Iqbal*, Ajmal Khan, Rashid Nazir, Shumaila Kiran, Shahnaz Perveen, Khalid M. Khan* and Muhammad I. Choudhary*   Pages 244 - 255 ( 12 )

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.

Affiliation:

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Department of Applied Chemistry, Government College University, Faisalabad-38000, Faisalabad, PCSIR Laboratories Complex Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi-75280, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270

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