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

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 st...

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Main Authors: Taha, Muhammad, Rahim, Faizal, Ali, Muhammad, Khan, Muhammad Naseem, Alqahtani, Mohammed A., Bamarouf, Yasser A., Gollapalli, Mohammed, Farooq, Rai Khalid, Ali Shah, Syed Adnan, Ahmed, Qamar Uddin, Zakaria, Zainul Amiruddin
Format: Article
Language:English
English
English
Published: MDPI 2019
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Online Access:http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/1/72570%20Synthesis%20of%20chromen-4-one-oxadiazole.pdf
http://irep.iium.edu.my/72570/2/72570%20Synthesis%20of%20chromen-4-one-oxadiazole%20SCOPUS.pdf
http://irep.iium.edu.my/72570/13/72570_Synthesis%20of%20Chromen-4-One-Oxadiazole%20Substituted%20Analogs%20as%20Potent%20-Glucuronidase%20Inhibitors_wos.pdf
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spelling iium-725702019-07-31T07:15:28Z http://irep.iium.edu.my/72570/ Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors Taha, Muhammad Rahim, Faizal Ali, Muhammad Khan, Muhammad Naseem Alqahtani, Mohammed A. Bamarouf, Yasser A. Gollapalli, Mohammed Farooq, Rai Khalid Ali Shah, Syed Adnan Ahmed, Qamar Uddin Zakaria, Zainul Amiruddin RS Pharmacy and materia medica 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. MDPI 2019-04 Article PeerReviewed application/pdf en http://irep.iium.edu.my/72570/1/72570%20Synthesis%20of%20chromen-4-one-oxadiazole.pdf application/pdf en http://irep.iium.edu.my/72570/2/72570%20Synthesis%20of%20chromen-4-one-oxadiazole%20SCOPUS.pdf application/pdf en http://irep.iium.edu.my/72570/13/72570_Synthesis%20of%20Chromen-4-One-Oxadiazole%20Substituted%20Analogs%20as%20Potent%20-Glucuronidase%20Inhibitors_wos.pdf 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 https://www.mdpi.com/1420-3049/24/8/1528 10.3390/molecules24081528
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
English
English
topic RS Pharmacy and materia medica
spellingShingle RS Pharmacy and materia medica
Taha, Muhammad
Rahim, Faizal
Ali, Muhammad
Khan, Muhammad Naseem
Alqahtani, Mohammed A.
Bamarouf, Yasser A.
Gollapalli, Mohammed
Farooq, Rai Khalid
Ali Shah, Syed Adnan
Ahmed, Qamar Uddin
Zakaria, Zainul Amiruddin
Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
description 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.
format Article
author Taha, Muhammad
Rahim, Faizal
Ali, Muhammad
Khan, Muhammad Naseem
Alqahtani, Mohammed A.
Bamarouf, Yasser A.
Gollapalli, Mohammed
Farooq, Rai Khalid
Ali Shah, Syed Adnan
Ahmed, Qamar Uddin
Zakaria, Zainul Amiruddin
author_facet Taha, Muhammad
Rahim, Faizal
Ali, Muhammad
Khan, Muhammad Naseem
Alqahtani, Mohammed A.
Bamarouf, Yasser A.
Gollapalli, Mohammed
Farooq, Rai Khalid
Ali Shah, Syed Adnan
Ahmed, Qamar Uddin
Zakaria, Zainul Amiruddin
author_sort Taha, Muhammad
title Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
title_short Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
title_full Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
title_fullStr Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
title_full_unstemmed Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
title_sort synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
publisher MDPI
publishDate 2019
url http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/
http://irep.iium.edu.my/72570/1/72570%20Synthesis%20of%20chromen-4-one-oxadiazole.pdf
http://irep.iium.edu.my/72570/2/72570%20Synthesis%20of%20chromen-4-one-oxadiazole%20SCOPUS.pdf
http://irep.iium.edu.my/72570/13/72570_Synthesis%20of%20Chromen-4-One-Oxadiazole%20Substituted%20Analogs%20as%20Potent%20-Glucuronidase%20Inhibitors_wos.pdf
first_indexed 2023-09-18T21:42:49Z
last_indexed 2023-09-18T21:42:49Z
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