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

13 Citations (Scopus)

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. This journal is

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

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Diacylglycerol O-Acyltransferase
Acrylamide
inhibitors
Derivatives
cultured cells
liver
rats
analogs
dosage
evaluation
synthesis
Hep G2 Cells
Microsomes
Liver
Rats
Triglycerides
Cells
Cell Line

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

Cite this

Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors. / Lee, Kyeong; Kim, Minkyoung; Lee, Boah; Goo, Jail; Kim, Jiyoung; Naik, Ravi; Seo, Jee Hee; Kim, Mun Ock; Byun, Youngjoo; Song, Gyu Yong; Lee, Hyun Sun; Choi, Yongseok.

In: Organic and Biomolecular Chemistry, Vol. 11, No. 5, 07.02.2013, p. 849-858.

Research output: Contribution to journalArticle

Lee, K, Kim, M, Lee, B, Goo, J, Kim, J, Naik, R, Seo, JH, Kim, MO, Byun, Y, Song, GY, Lee, HS & Choi, Y 2013, 'Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors', Organic and Biomolecular Chemistry, vol. 11, no. 5, pp. 849-858. https://doi.org/10.1039/c2ob27114a
Lee, Kyeong ; Kim, Minkyoung ; Lee, Boah ; Goo, Jail ; Kim, Jiyoung ; Naik, Ravi ; Seo, Jee Hee ; Kim, Mun Ock ; Byun, Youngjoo ; Song, Gyu Yong ; Lee, Hyun Sun ; Choi, Yongseok. / Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors. In: Organic and Biomolecular Chemistry. 2013 ; Vol. 11, No. 5. pp. 849-858.
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