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

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Title
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
Author(s)
A Gelain; I Bettinelli; D Barlocco; Byoung-Mog Kwon; Tae Sook Jeong; Kyung Hyun Cho; L Toma
Bibliographic Citation
Journal of Medicinal Chemistry, vol. 48, no. 24, pp. 7708-7713
Publication Year
2005
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.
ISSN
0022-2623
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/jm050703x
Type
Article
Appears in Collections:
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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