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Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent ?-Glucuronidase Inhibitors.


ABSTRACT: Chromen-4-one substituted oxadiazole analogs 1-19 have been synthesized, characterized and evaluated for ?-glucuronidase inhibition. All analogs exhibited a variable degree of ?-glucuronidase inhibitory activity with IC50 values ranging in between 0.8 ± 0.1-42.3 ± 0.8 ?M when compared with the standard d-saccharic acid 1,4 lactone (IC50 = 48.1 ± 1.2 ?M). 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.

SUBMITTER: Taha M 

PROVIDER: S-EPMC6514607 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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