Apotentialdualinhibitor(4)forexogenousabsorptionandendogenicsynthesisofcholesterolwasdesignedbasedontheconjugationoftheβ-lactampharmacophoreofezetimibeandtheδ-lactonepharmacophoreofstatins.Themergerofezetimibeandstatin4wassynthesizedfromp-hydroxybenzaldehydethroughaten-steproute.1HNMRanalysisshowedexistenceoffourpairsofenantiomers(5.7:5.7:1:1,molarratio).Andcompound4wasfoundtolowertotalglucose(TG)levelinratserumviaahigh-cholesterolandhigh-fatfeedingexperiment.
