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Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors
- Lee, Kyeong;
- Kim, Minkyoung;
- Lee, Boah;
- Goo, Jail;
- Kim, Jiyoung;
- 외 7명
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15초록
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.
키워드
TRIGLYCERIDE SYNTHESIS; DGAT1 INHIBITORS; POTENT; OBESITY; ACID; MICE; BIOSYNTHESIS; TARGET
- 제목
- Discovery of indolyl acrylamide derivatives as human diacylglycerol acyltransferase-2 selective inhibitors
- 저자
- 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
- 발행일
- 2013-02-07
- 유형
- Article
- 권
- 11
- 호
- 5
- 페이지
- 849 ~ 858