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

2 Citations (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

Keywords

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

ASJC Scopus subject areas

  • Chemistry(all)

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