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Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase-1 Inhibitors
- Authors
- Kim, Minkyoung; Kwon, Jinsun; Kim, Mun Ock; Singh, Sarbjit; Kim, Sang Kyum; Lee, Kyeong; Lee, Kiho; Lee, Hyun Sun; Choi, Yongseok
- Issue Date
- Feb-2015
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- Diacylglycerol O-acyltransferase inhibitor; Triglyceride; Obesity; Hydrazide; Diacylglycerol O-acyltransferase
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.36, no.2, pp 628 - 635
- Pages
- 8
- Indexed
- SCI
SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 36
- Number
- 2
- Start Page
- 628
- End Page
- 635
- ISSN
- 0253-2964
1229-5949
- 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.
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Related Researcher
- Lee, Kyeong
- College of Pharmacy (Department of Pharmacy)