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Mono- or diphenylpyridazines connected to N-(2,4-difluorophenyl)-N'-heptylurea as acyl-CoA:cholesterol acyltransferase inhibitors.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Gelain A,Bettinelli I,Barlocco D,Kwon BM,Jeong TS,Cho KH,Toma L

doi

10.1021/jm050703x

keywords:

subject

Has Abstract

pub_date

2005-12-01 00:00:00

pages

7708-13

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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