2. Academic Validation
  3. Synthesis and β-glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones

Synthesis and β-glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones

  • Bioorg Med Chem. 2014 Jul 1;22(13):3449-54. doi: 10.1016/j.bmc.2014.04.039.
Khalid Mohammed Khan 1,  Syed Muhammad Saad 2,  Nimra Naveed Shaikh 2,  Shafqat Hussain 2,  Muhammad Imran Fakhri 2,  Shahnaz Perveen 3,  Muhammad Taha 4,  Muhammad Iqbal Choudhary 5
Affiliations

Affiliations

  • 1 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. Electronic address: hassaan2@super.net.pk.
  • 2 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • 3 PCSIR Laboratories Complex, Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi 75280, Pakistan.
  • 4 Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Puncak Alam Campus, 42300, Malaysia.
  • 5 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan; Department of Biochemistry, Faculty of Sciences, King Abdulaziz University, Jeddah 2254, Saudi Arabia.
PMID: 24844756 DOI: 10.1016/j.bmc.2014.04.039
Abstract

2-Arylquinazolin-4(3H)-ones 1-25 were synthesized by reacting anthranilamide with various benzaldehydes using CuCl2·2H2O as a catalyst in ethanol under reflux. Synthetic 2-arylquinazolin-4(3H)-ones 1-25 were evaluated for their β-glucuronidase inhibitory potential. A trend of inhibition IC50 against the Enzyme in the range of 0.6-198.2μM, was observed and compared with the standard d-saccharic acid 1,4-lactone (IC50=45.75±2.16μM). Compounds 13, 19, 4, 12, 14, 22, 23, 25, 15, 8, 17, 11, 21, 1, 3, 18, 9, 2, and 24 with the IC50 values within the range of 0.6-44.0μM, indicated that the compounds have superior activity than the standard. The compounds showed no cytotoxic effects against PC-3 cells. A structure-activity relationship is established.

Keywords

2-Arylquinazolin-4(3H)-ones; Cytotoxicity; Structure–activity relationship; β-Glucuronidase inhibition.

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