Issue 5, 2013
From the journal:

Organic & Biomolecular Chemistry

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

Kyeong Lee,‡a   Minkyoung Kim,‡b   Boah Lee,b   Jail Goo,b   Jiyoung Kim,b   Ravi Naik,a   Jee Hee Seo,c   Mun Ock Kim,c   Youngjoo Byun,d   Gyu-Yong Song,e   Hyun Sun Lee*c  and  Yongseok Choi*b  

* Corresponding authors

a College of Pharmacy, Dongguk University-Seoul, Seoul 100-715, Korea

b College of Life Sciences and Biotechnology, Korea University, Seoul 136-701, Korea
E-mail: ychoi@korea.ac.kr
Fax: +82-2-3290-3650
Tel: +82-2-3290-3650

c Chemical Biology Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, Chungbuk 363-883, Korea
E-mail: leehs@kribb.re.kr

d College of Pharmacy, Korea University, Chungnam 339-700, Korea

e College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea

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.

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

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Article information

DOI
https://doi.org/10.1039/C2OB27114A
Article type
Paper
Submitted
30 Oct 2012
Accepted
28 Nov 2012
First published
29 Nov 2012

Org. Biomol. Chem., 2013,11, 849-858

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

K. Lee, M. Kim, B. Lee, J. Goo, J. Kim, R. Naik, J. H. Seo, M. O. Kim, Y. Byun, G. Song, H. S. Lee and Y. Choi, Org. Biomol. Chem., 2013, 11, 849 DOI: 10.1039/C2OB27114A

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