Discovery of a Novel Series of Indolyl Hydrazide Derivatives as Diacylglycerol Acyltransferase‐1 Inhibitors. (23rd January 2015)

• Record Type: Journal Article
• Authors: Kim, Minkyoung; Kwon, Jinsun; Kim, Mun Ock; Singh, Sarbjit; Kim, Sang Kyum; Lee, Kyeong; Lee, Kiho; Lee, Hyun Sun; Choi, Yongseok
• Is Part Of: Bulletin of the Korean Chemical Society. Volume 36:Number 2(2015:Feb.)
• Page Start: 628
• Page End: 635
• Publication Date: 2015-01-23
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1002/bkcs.10123
• Languages: English
• ISSNs: 0253-2964

Abstract

<abstract abstract-type="main" id="bkcs10123-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p id="bkcs10123-para-0001">A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds <bold>8u</bold> and <bold>8v</bold> exhibited selective and potent DGAT‐1 inhibitory activities. In addition, compound <bold>8u</bold> dose‐dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound <bold>8u</bold> 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.</p> </abstract>