Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase-1 Inhibitors

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 cel...

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Veröffentlicht in:Bulletin of the Korean Chemical Society 2015, 36(2), , pp.628-635
Hauptverfasser: Kim, Minkyoung, Kwon, Jinsun, Kim, Mun Ock, Singh, Sarbjit, Kim, Sang Kyum, Lee, Kyeong, Lee, Kiho, Lee, Hyun Sun, Choi, Yongseok
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Sprache:eng
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Zusammenfassung: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.
ISSN:1229-5949
0253-2964
1229-5949
DOI:10.1002/bkcs.10123