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Chromen-4-one substituted oxadiazole analogs - have been synthesized, characterized and evaluated for -glucuronidase inhibition. All analogs exhibited a variable degree of -glucuronidase inhibitory activity with IC values ranging in between 0.8 ± 0.1-42.3 ± 0.8 μM when compared with the standard d-saccharic acid 1,4 lactone (IC = 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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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6514607PMC
http://dx.doi.org/10.3390/molecules24081528DOI Listing

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

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April 2019

Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia.

Chromen-4-one substituted oxadiazole analogs - have been synthesized, characterized and evaluated for -glucuronidase inhibition. All analogs exhibited a variable degree of -glucuronidase inhibitory activity with IC values ranging in between 0.8 ± 0.

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