European Journal of Medicinal Chemistry p. 377 - 386 (1995)
Update date:2022-08-04
Topics:
Nioche, J. Y.
Decerprit, J.
Festal, D.
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
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