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Title 

Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

Authors 

K LeeM KimB LeeJ GooJ KimR NaikJee Hee SeoMun-Ock KimY ByunG Y SongHyun Sun LeeY Choi

Publisher 

Royal Society of Chemistry

Issue Date 

2013

Citation 

Organic & Biomolecular Chemistry, vol. 11, no. 5, pp. 849-858

Abstract 

A series of indolyl acrylamide derivatives was synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Furfurylamine containing indolyl acrylamide derivative 5h exhibited the most potent DGAT inhibitory activity using microsomes prepared from rat liver. Further evaluation against human DGAT-1 and DGAT-2 identified indolyl acrylamide analogues as selective inhibitors against human DGAT-2. In addition, the most potent compound 5h inhibited triglyceride synthesis dose-dependently in HepG2 cell lines.

ISSN 

1477-0520

Link 

http://dx.doi.org/10.1039/c2ob27114a

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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