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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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 |
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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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1777413253669847040 |