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- Title
Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase-1 Inhibitors.
- Authors
Minkyoung Kim; Jinsun Kwon; Sarbjit Singh; Yongseok Choi; Mun Ock Kim; Hyun Sun Lee; Sang Kyum Kim; Kyeong Lee; Kiho Lee
- Abstract
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.
- Subjects
DIGLYCERIDES; ENZYME inhibitors; TRIGLYCERIDES; OBESITY treatment; HYDRAZIDES
- Publication
Bulletin of the Korean Chemical Society, 2015, Vol 36, Issue 2, p628
- ISSN
0253-2964
- Publication type
Article
- DOI
10.1002/bkcs.10123