Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives

We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferase‐1 (DGAT)‐1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGAT‐1, selectivity toward DGAT‐2, and liver microsomal stability. Compound 6b exhib...

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Published in:Bulletin of the Korean Chemical Society 2015, 36(6), , pp.1586-1593
Main Authors: Han, Seo-Jung, Lee, Gwi Bin, Kwak, Hyun Jung, Pagire, Suvarna H., Kim, Ji Young, Pagire, Haushabhau S., Park, Sung Bum, Chae, Chong Hak, Lee, Joo Yun, Kim, Ki Young, Rhee, Sang Dal, Kim, Hee Youn, Shin, Sun Hye, Bae, Myung Ae, Park, Mi-jin, Kim, Dooseop, Lee, Duck Hyung, Ahn, Jin Hee
Format: Article
Language:English
Subjects:
3-Azabicyclo[3.1.0]hexane
Diacylglycerol acyltransferase-1
Oral lipid tolerance test
Triglycerides
화학
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Summary:We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferase‐1 (DGAT)‐1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGAT‐1, selectivity toward DGAT‐2, and liver microsomal stability. Compound 6b exhibited no CYP inhibition, hERG binding, or cell cytotoxicity. Additionally, compound 6b reduced the level of plasma triglyceride after oral administration in mice.
ISSN:1229-5949
0253-2964
1229-5949
DOI:10.1002/bkcs.10302