The Design And Synthesis Of The ¦Á-phenyl Methylene-¦Â-oxo-benzenepropanoic Acid Derivative

The pathogenic mechanism of diabetic complications and the advances in aldose reductase (AR) inhibitors are reviewed briefly in this thesis. It has been reported that hyperactivity of the polyol pathway induces or contributes to the progressing of diabetic complications and inhibitors of AR can prevent or treat complications of diabetes mellitus.The aim of our study is to find new AR inhibitors. Based on the foundmental structure of chalcone compounds having AR inhibitory activities and the molecular action mechanism of known ARIs,α-(phenylmethylene)-β-oxo-benzenepropanoic acid derivatives were designed. Starting from acetophenone or substituted acetophenone, nineteen compounds were obtained via Claisen condensation, Knoenvernagel condensation and hydrolization, and all of them are not reported in the literatures. The structures of target compounds were characterized by ~1H-NMR and IR.