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Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors


Taha, Muhammad and Rahim, Fazal and Ali, Muhammad and Khan, Muhammad Naseem and Alqahtani, Mohammed A. and Bamarouf, Yasser A. and Gollapalli, Mohammed and Farooq, Rai Khalid and Shah, Syed Adnan Ali and Ahmed, Qamar Uddin and Zakaria, Zainul Amiruddin (2019) Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors. Molecules, 24 (8). art. no. 1528. pp. 1-13. ISSN 1420-3049


Chromen-4-one substituted oxadiazole analogs 1–19 have been synthesized, characterized and evaluated for β-glucuronidase inhibition. All analogs exhibited a variable degree of β-glucuronidase inhibitory activity with IC50 values ranging in between 0.8 ± 0.1–42.3 ± 0.8 μM when compared with the standard d-saccharic acid 1,4 lactone (IC50 = 48.1 ± 1.2 μM). Structure activity relationship has been established for all compounds. Molecular docking studies were performed to predict the binding interaction of the compounds with the active site of enzyme.

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Official URL or Download Paper: https://www.mdpi.com/1420-3049/24/8/1528

Additional Metadata

Item Type: Article
Divisions: Faculty of Medicine and Health Science
Halal Products Research Institute
DOI Number: https://doi.org/10.3390/molecules24081528
Publisher: MDPI
Keywords: Chromen-4-one; Oxadiazole; Synthesis; β-glucuronidase inhibition; Molecular docking; SAR
Depositing User: Nabilah Mustapa
Date Deposited: 04 May 2020 16:26
Last Modified: 04 May 2020 16:26
Altmetrics: http://www.altmetric.com/details.php?domain=psasir.upm.edu.my&doi=10.3390/molecules24081528
URI: http://psasir.upm.edu.my/id/eprint/38388
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