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...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English English English |
| Published: |
MDPI
2019
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| Subjects: | |
| 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 |
| Summary: | 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. |
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