Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors

Minkyoung Kim, Jinsun Kwon, Mun Ock Kim, Sarbjit Singh, Sang Kyum Kim, Kyeong Lee, Kiho Lee, Hyun Sun Lee, Yongseok Choi

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.

Original languageEnglish
Pages (from-to)628-635
Number of pages8
JournalBulletin of the Korean Chemical Society
Volume36
Issue number2
DOIs
Publication statusPublished - 2015 Feb 20

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Diacylglycerol O-Acyltransferase
Triglycerides
Derivatives
Lipids
Animals
Cells
Plasmas

Keywords

  • Diacylglycerol O-acyltransferase
  • Diacylglycerol O-acyltransferase inhibitor
  • Hydrazide
  • Obesity
  • Triglyceride

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors. / Kim, Minkyoung; Kwon, Jinsun; Kim, Mun Ock; Singh, Sarbjit; Kim, Sang Kyum; Lee, Kyeong; Lee, Kiho; Lee, Hyun Sun; Choi, Yongseok.

In: Bulletin of the Korean Chemical Society, Vol. 36, No. 2, 20.02.2015, p. 628-635.

Research output: Contribution to journalArticle

Kim, Minkyoung ; Kwon, Jinsun ; Kim, Mun Ock ; Singh, Sarbjit ; Kim, Sang Kyum ; Lee, Kyeong ; Lee, Kiho ; Lee, Hyun Sun ; Choi, Yongseok. / Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors. In: Bulletin of the Korean Chemical Society. 2015 ; Vol. 36, No. 2. pp. 628-635.
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