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Issue 5, 2013
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Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors

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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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Publication details

The article was received on 30 Oct 2012, accepted on 28 Nov 2012 and first published on 29 Nov 2012


Article type: Paper
DOI: 10.1039/C2OB27114A
Citation: 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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