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...
| Published in: | Molecules |
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| Format: | Article |
| Language: | English |
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MDPI AG
2019
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85064857181&doi=10.3390%2fmolecules24081528&partnerID=40&md5=e34c1777a234ed865eb8f914ee260af5 |
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2-s2.0-85064857181 |
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2-s2.0-85064857181 Taha M.; Rahim F.; Ali M.; Khan M.N.; Alqahtani M.A.; Bamarouf Y.A.; Gollapalli M.; Farooq R.K.; Ali Shah S.A.; Ahmed Q.U.; Zakaria Z.A. Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors 2019 Molecules 24 8 10.3390/molecules24081528 https://www.scopus.com/inward/record.uri?eid=2-s2.0-85064857181&doi=10.3390%2fmolecules24081528&partnerID=40&md5=e34c1777a234ed865eb8f914ee260af5 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. © 2019 by the authors. MDPI AG 14203049 English Article All Open Access; Gold Open Access |
| author |
Taha M.; Rahim F.; Ali M.; Khan M.N.; Alqahtani M.A.; Bamarouf Y.A.; Gollapalli M.; Farooq R.K.; Ali Shah S.A.; Ahmed Q.U.; Zakaria Z.A. |
| spellingShingle |
Taha M.; Rahim F.; Ali M.; Khan M.N.; Alqahtani M.A.; Bamarouf Y.A.; Gollapalli M.; Farooq R.K.; Ali Shah S.A.; Ahmed Q.U.; Zakaria Z.A. Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors |
| author_facet |
Taha M.; Rahim F.; Ali M.; Khan M.N.; Alqahtani M.A.; Bamarouf Y.A.; Gollapalli M.; Farooq R.K.; Ali Shah S.A.; Ahmed Q.U.; Zakaria Z.A. |
| author_sort |
Taha M.; Rahim F.; Ali M.; Khan M.N.; Alqahtani M.A.; Bamarouf Y.A.; Gollapalli M.; Farooq R.K.; Ali Shah S.A.; Ahmed Q.U.; Zakaria Z.A. |
| 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 |
| publishDate |
2019 |
| container_title |
Molecules |
| container_volume |
24 |
| container_issue |
8 |
| doi_str_mv |
10.3390/molecules24081528 |
| url |
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85064857181&doi=10.3390%2fmolecules24081528&partnerID=40&md5=e34c1777a234ed865eb8f914ee260af5 |
| 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. © 2019 by the authors. |
| publisher |
MDPI AG |
| issn |
14203049 |
| language |
English |
| format |
Article |
| accesstype |
All Open Access; Gold Open Access |
| record_format |
scopus |
| collection |
Scopus |
| _version_ |
1814778506970660864 |