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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

Authors 

A GelainD BarloccoByoung-Mog KwonTae Sook JeongK R ImL LegnaniL Toma

Publisher 

American Chemical Society

Issue Date 

2008

Citation 

Journal of Medicinal Chemistry, vol. 51, no. 5, pp. 1474-1477

Keywords 

cholesterol acyltransferase inhibitor biphenyl derivativecholesterol acyltransferase inhibitor phenylpyridazine derivativebiphenyl compounds

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

Link 

http://dx.doi.org/10.1021/jm701474c

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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