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Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase-1 Inhibitors
- Kim, Minkyoung;
- Kwon, Jinsun;
- Kim, Mun Ock;
- Singh, Sarbjit;
- Kim, Sang Kyum;
- ... Lee, Kyeong;
- 외 3명
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2초록
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.
키워드
Diacylglycerol O-acyltransferase inhibitor; Triglyceride; Obesity; Hydrazide; Diacylglycerol O-acyltransferase; OPTIMIZATION; POTENT
- 제목
- Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase-1 Inhibitors
- 저자
- Kim, Minkyoung; Kwon, Jinsun; Kim, Mun Ock; Singh, Sarbjit; Kim, Sang Kyum; Lee, Kyeong; Lee, Kiho; Lee, Hyun Sun; Choi, Yongseok
- 발행일
- 2015-02
- 유형
- Article
- 권
- 36
- 호
- 2
- 페이지
- 628 ~ 635