Mono- or diphenylpyridazines connected to N-(2,4-Difluorophenyl)-N'-heptylurea as acyl-CoA:cholesterol acyltransferase inhibitors = 피라진계 화합물의 ACAT 저해활성 및 구조-활성 관계

Abstract

Mono- and diphenylpyridazine ureido derivatives, structurally related to DuP 128, were synthesized and tested for their inhibitory activity against ACAT isolated from rat liver microsomes. Several compounds displayed ACAT inhibition in the micromolar range. The amino derivatives 4a-c were also tested against hACAT-1 and hACAT-2 isoforms. They retained the same trend shown in the previous assay. Modeling studies on representative terms were performed. Significant similarities between the geometrical features of the model DuP 128 and the most active pyridazine derivatives were observed.