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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and β-glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones
Bioorganic and Medicinal Chemistry, Volume 22, No. 13, Year 2014
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Description
2-Arylquinazolin-4(3H)-ones 1-25 were synthesized by reacting anthranilamide with various benzaldehydes using CuCl2·2H 2O 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 0.6-198.2 μM, was observed and compared with the standard d-saccharic acid 1,4-lactone (IC50 = 45.75 ± 2.16 μM). 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 0.6-44.0 μM, 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. © 2014 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Khan, K. M.
Pakistan, Karachi
University of Karachi
Saad, Syed Muhammad
Pakistan, Karachi
University of Karachi
Shaikh, Nimra Naveed
Pakistan, Karachi
University of Karachi
Hussain, Sabbir M.Shakil
Pakistan, Karachi
University of Karachi
Fakhri, Muhammad Imran
Pakistan, Karachi
University of Karachi
Perveen, Shahnaz
Pakistan, Peshawar
Pcsir Laboratories
Taha, Muhammad
Malaysia, Shah Alam
Universiti Teknologi Mara
Choudhary, Mohammed Iqbal
Pakistan, Karachi
University of Karachi
Saudi Arabia, Jeddah
King Abdulaziz University
Statistics
Citations: 58
Authors: 8
Affiliations: 4
Identifiers
Doi:
10.1016/j.bmc.2014.04.039
ISSN:
09680896
e-ISSN:
14643391