Abstract: To study the synthesis and cholesterol-absorption inhibitory activity of novel lipid-regulating agents with monocyclic β-lactam.The target compounds were prepared in five steps via monoesterification,acylation,Staudinger ketene-imine cycloaddition,hydrolysis,and incorporation with furoxans or nitrates,using glutaric anhydride as the starting material.The cholesterol absorption inhibition activities were assessed using 72-day cholesterol-fed hamster model.The structures of thirteen target compounds were confirmed by MS,1H NMR,IR and element analysis.Preliminary results showed that all the compounds except compound 2c possessed cholesterol-absorption inhibitory activity to a different extent,and compound 2g was the most potent one within this series of compounds.