Details

Autor(en) / Beteiligte

• 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

Titel

Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitorsElectronic supplementary information (ESI) available. See DOI: 10.1039/c2ob27114a

Erscheinungsjahr

2013-01

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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. A novel series of indolyl acrylamide derivatives was synthesized as DGAT inhibitors, identifying compound 5h as a selective hDGAT-2 inhibitor with an IC 50 value of 6.9 μM.