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

Kyeong Lee, Minkyoung Kim, Boah Lee, Jail Goo, Jiyoung Kim, Ravi Naik, Jee Hee Seo, Mun Ock Kim, Youngjoo Byun, Gyu Yong Song, Hyun Sun Lee, Yongseok Choi

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)849-858
Number of pages10
JournalOrganic and Biomolecular Chemistry
Volume11
Issue number5
DOIs
StatePublished - Feb 7 2013
Externally publishedYes

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

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  • Cite this

    Lee, K., Kim, M., Lee, B., Goo, J., Kim, J., Naik, R., Seo, J. H., Kim, M. O., Byun, Y., Song, G. Y., Lee, H. S., & Choi, Y. (2013). Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors. Organic and Biomolecular Chemistry, 11(5), 849-858. https://doi.org/10.1039/c2ob27114a