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

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Title
Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors
Author(s)
K Lee; M Kim; B Lee; J Goo; J Kim; R Naik; Jee Hee Seo; Mun-Ock Kim; Y Byun; G Y Song; Hyun Sun Lee; Y Choi
Bibliographic Citation
Organic & Biomolecular Chemistry, vol. 11, no. 5, pp. 849-858
Publication Year
2013
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
Publisher
Royal Soc Chem
DOI
http://dx.doi.org/10.1039/c2ob27114a
Type
Article
Appears in Collections:
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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