Synthesis and structure-activity relationships of new ACAT inhibitors

Article abstract of DOI:10.1016/0223-5234(96)88247-X

A series of heterocyclic ureas were synthesized and their ability to inhibit arterial and intestinal ACAT was assessed in animals.The structural modifications carried out in this series led to N2-(2,4-difluorophenyl)-N₁-8-(4-fluorophenyl)-2,3,4,5-tetrahydro-1-benzoxepin-5-yl-N₁-n-heptylurea 21, which proved to be very active on both the inhibition of aortic ACAT and the inhibition of rat cholesterol intestinal absorption, thus exhibiting a strong hypocholesterolemic effect po in rat (ED25 = 0.2 mg/kg). aortic ACAT / intestinal inhibition / benzoxepin / urea / cholesterol / hypocholesterolaemic activity