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Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors
- Authors
- 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
- Issue Date
- 2013
- Publisher
- ROYAL SOC CHEMISTRY
- Citation
- ORGANIC & BIOMOLECULAR CHEMISTRY, v.11, no.5, pp.849 - 858
- Indexed
- SCIE
SCOPUS
- Journal Title
- ORGANIC & BIOMOLECULAR CHEMISTRY
- Volume
- 11
- Number
- 5
- Start Page
- 849
- End Page
- 858
- ISSN
- 1477-0520
- 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.
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