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 stand...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI
2019
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| Online Access: | http://psasir.upm.edu.my/id/eprint/38388/ http://psasir.upm.edu.my/id/eprint/38388/1/38388.pdf |
| _version_ | 1848848865912946688 |
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| author | Taha, Muhammad Rahim, Fazal Ali, Muhammad Khan, Muhammad Naseem Alqahtani, Mohammed A. Bamarouf, Yasser A. Gollapalli, Mohammed Farooq, Rai Khalid Shah, Syed Adnan Ali Ahmed, Qamar Uddin Zakaria, Zainul Amiruddin |
| author_facet | Taha, Muhammad Rahim, Fazal Ali, Muhammad Khan, Muhammad Naseem Alqahtani, Mohammed A. Bamarouf, Yasser A. Gollapalli, Mohammed Farooq, Rai Khalid Shah, Syed Adnan Ali Ahmed, Qamar Uddin Zakaria, Zainul Amiruddin |
| author_sort | Taha, Muhammad |
| building | UPM Institutional Repository |
| collection | Online Access |
| 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. |
| first_indexed | 2025-11-15T09:41:18Z |
| format | Article |
| id | upm-38388 |
| institution | Universiti Putra Malaysia |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T09:41:18Z |
| publishDate | 2019 |
| publisher | MDPI |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | upm-383882020-05-04T16:26:37Z http://psasir.upm.edu.my/id/eprint/38388/ Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors Taha, Muhammad Rahim, Fazal Ali, Muhammad Khan, Muhammad Naseem Alqahtani, Mohammed A. Bamarouf, Yasser A. Gollapalli, Mohammed Farooq, Rai Khalid Shah, Syed Adnan Ali Ahmed, Qamar Uddin Zakaria, Zainul Amiruddin 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 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/38388/1/38388.pdf 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 https://www.mdpi.com/1420-3049/24/8/1528 10.3390/molecules24081528 |
| spellingShingle | Taha, Muhammad Rahim, Fazal Ali, Muhammad Khan, Muhammad Naseem Alqahtani, Mohammed A. Bamarouf, Yasser A. Gollapalli, Mohammed Farooq, Rai Khalid Shah, Syed Adnan Ali Ahmed, Qamar Uddin Zakaria, Zainul Amiruddin Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors |
| title | 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_short | 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 |
| url | http://psasir.upm.edu.my/id/eprint/38388/ http://psasir.upm.edu.my/id/eprint/38388/ http://psasir.upm.edu.my/id/eprint/38388/ http://psasir.upm.edu.my/id/eprint/38388/1/38388.pdf |