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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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
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 |
| 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. © 2019 by the authors. |
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| ISSN: | 14203049 |
| DOI: | 10.3390/molecules24081528 |