Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 11, Issue 5, Pages 849-858Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob27114a
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Funding
- KRIBB Research Initiative Program
- Basic Science Research Program through the National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2010-0024662, 2012053532]
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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.
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