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

Taha, Muhammad and Rahim, Faizal and Ali, Muhammad and Khan, Muhammad Naseem and Alqahtani, Mohammed A. and Bamarouf, Yasser A. and Gollapalli, Mohammed and Farooq, Rai Khalid and Ali Shah, Syed Adnan 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). pp. 1-13. ISSN 1420-3049

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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.

Item Type: Article (Journal)
Additional Information: 4921/72570
Uncontrolled Keywords: chromen-4-one; oxadiazole; synthesis; β-glucuronidase inhibition; molecular docking; SAR
Subjects: R Medicine > RS Pharmacy and materia medica
Kulliyyahs/Centres/Divisions/Institutes: Kulliyyah of Pharmacy
Kulliyyah of Pharmacy > Department of Pharmaceutical Chemistry
Depositing User: Dr Qamar Uddin Ahmed
Date Deposited: 12 Jun 2019 14:54
Last Modified: 31 Jul 2019 15:15
URI: http://irep.iium.edu.my/id/eprint/72570

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