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RSS FeedsMolecules, Vol. 24, Pages 1528: Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent ?-Glucuronidase Inhibitors (Molecules)

 
 

18 april 2019 14:03:19

 
Molecules, Vol. 24, Pages 1528: Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent ?-Glucuronidase Inhibitors (Molecules)
 




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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44 viewsCategory: Biochemistry, Chemistry, Molecular Biology
 
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