Design, synthesis, and urease inhibition activities of some bis-coumarin-perimidine hybrid compounds

Abstract

A series of bis-coumarin-perimidine hybrids were designed and synthesized, and their structures were characterized by FT-IR, H-1 NMR, C-13 NMR, and elemental analyses spectral data. All newly synthesized compounds were screened for their urease activity. All synthesized compounds were found to be effective in urease enzyme inhibition. With IC50 values ranging from 0.022 +/- 0.50 to 0.098 +/- 0.10 mu M, the compounds exhibit more active inhibition than the standard thiourea (IC50 = 0.206 +/- 0.25 mu M). The compound N ',N ''-(2,2 '-(2,2 '-(2-oxo-1H-perimidine-1,3(2H)-diyl)bis(acetyl))bis(6-bromo-2-oxo-2H-chromene-3-carbohydrazide) has the best urease inhibition with IC50 = 0.022 +/- 0.50 mu M.