Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of Acyl-CoA:cholesterol acyl transferase inhibitors = 바이페닐계와 페닐피라진계간의 활성 비교 분석

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Title
Biphenyl versus phenylpyridazine derivatives: the role of the heterocycle in a series of Acyl-CoA:cholesterol acyl transferase inhibitors = 바이페닐계와 페닐피라진계간의 활성 비교 분석
Author(s)
A Gelain; D Barlocco; Byoung-Mog Kwon; Tae Sook Jeong; K R Im; L Legnani; L Toma
Bibliographic Citation
Journal of Medicinal Chemistry, vol. 51, no. 5, pp. 1474-1477
Publication Year
2008
Abstract
A series of alkylamido- (1) and alkylaminobiphenyl (2) derivatives were synthesized as possible bioisosters of the reported ACAT inhibitors phenylpyridazine analogues (I). Both 1 and 2 were tested on the human ACAT-1 and ACAT-2 isoforms. The amino derivatives 2 were found to be inactive, contrary to the related pyridazine derivatives. By contrast, the ortho-substituted amides la and Id showed an interesting activity. These results support the essential role of the pyridazine nucleus. Modeling studies were also performed.
ISSN
0022-2623
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/jm701474c
Type
Article
Appears in Collections:
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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