Fork Base, ¦Á-benzyl-¦Â-oxo-phenylpropionate Derivatives Design And Synthesis And Aldose Reductase Inhibitory Activity

The pathogenic mechanism of diabetic complications and the advances in aldose reductase (AR) inhibitors were briefly reviewed 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 and synthesized. Fifteen compounds were obtained and 13 of them were new ones. The structures of them were characterized by ¹H-NMR and IR. Their AR inhibitory activities were evaluated on rat lens aldose reductase . Compound 110 (80.48% inhibition at 10^-4mol/L) showed good activities.