Citation
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
Abstract
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
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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 |
| Statistic Details: | View Download Statistic |
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