Using structure-based basic screening approach, a coumarin acquired was articular as β-glucuronidase inhibitor. A focused library of coumarin derivatives was actinic by eco-benign adaptation of actinic reaction, and all constructed compounds were characterized by application spectroscopy. These compounds were begin to be inhibitor of β-glucuronidase with IC50 ethics in a micromolar range. All constructed compounds apparent absorbing inhibitory action adjoin β-glucuronidase, however, their authority assorted essentially from IC50 = 9.9–352.6 μM. Of twenty-one compounds, four apparent a bigger inhibitory contour than the antecedent hit 1.