β-Glucuronidase Inhibitory Studies on Coumarin Derivatives

Title:β-Glucuronidase Inhibitory Studies on Coumarin Derivatives

Volume: 10 Issue: 8

Author(s): Khalid Mohammed Khan, Muhammad Imran Fakhri, Nimra Naveed Shaikh, Syed Muhammad Saad, Shafqat Hussain, Shahnaz Perveen and Muhammad Iqbal Choudhary

Affiliation:

Keywords: β-glucuronidase, coumarin, Pechmann reaction, enzyme inhibition, β-glucuronidase related disorders, acid catalysis.

Abstract: Twenty-three (23) derivatives of coumarin (5-27) were synthesized and screened for their in vitro β- glucuronidase (E. coli) inhibitory activities. Only three compounds, 7,8-dihydroxy-4-methyl-2H-chromen-2-one (9) (IC₅₀ = 52.39 ± 1.85 µM), 3-chloro-6-hexyl-7-hydroxy-4-methyl-2H-chromen-2-one (18) (IC₅₀ = 60.50 ± 0.87 µM), and 3,6- dichloro-7-hydroxy-4-methyl-2H-chromen-2-one (15) (IC₅₀ = 380.26 ± 0.92 µM) displayed activities against β- glucuronidase as compared to standard D-saccharic acid 1,4-lactone (IC₅₀ = 45.75 ± 2.16 µM). The results indicated that the activity of the synthetic coumarins depends upon the substituents present on the coumarin skeleton.

Cite this article as:

Khan Mohammed Khalid, Fakhri Imran Muhammad, Shaikh Naveed Nimra, Saad Muhammad Syed, Hussain Shafqat, Perveen Shahnaz and Choudhary Iqbal Muhammad, β-Glucuronidase Inhibitory Studies on Coumarin Derivatives, Medicinal Chemistry 2014; 10 (8) . https://dx.doi.org/10.2174/1573406410666140311093352