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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

Authors 

A GelainI BettinelliD BarloccoByoung-Mog KwonTae Sook JeongKyung Hyun ChoL Toma

Publisher 

American Chemical Society

Issue Date 

2005

Citation 

Journal of Medicinal Chemistry, vol. 48, no. 24, pp. 7708-7713

Keywords 

cholesterol acyltransferasecholesterol acyltransferase inhibitorsterol o-acyltransferase

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

Link 

http://dx.doi.org/10.1021/jm050703x

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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