Abstract
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.
Highlights
Introduction βGlucuronidase (E.C.3.2.1.31) is one of the most extensively studied enzymes in the metabolic hydrolysis of conjugated compounds, and eliminates large number of toxic compounds from body as glucuronides [1]
Bacterialβ-glucuronidase β-glucuronidaseand andβ-glucosidase β-glucosidasein inthe the human human colon colon bladder and breast cancers are involved in the metabolism and activation of xenobiotics derived from dietary compounds are involved in the metabolism and activation of xenobiotics derived from dietary compounds [10]
The structure activity relationship has been established on the basis of substitution pattern on the phenyl ring
Summary
2-hydroxyacetophenone potassium hydroxide at at room room temperature temperature (Scheme (Scheme 1). Synthesis of chromene based oxadiazole derivatives 1–19
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
