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

Title
Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives
Authors
한서정Gwi Bin LeeHyun Jung KwakSuvarna H. PagireJi Young KimHaushabhau S. PagireSung Bum ParkChong Hak ChaeJoo Yun LeeKi Young KimSang Dal RheeHee Youn KimSun Hye ShinMyung Ae BaeMi-Jin ParkDooseop KimDuck Hyung LeeJin Hee Ahn
Issue Date
2015-06
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 36, NO 6-1593
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/67372
ISSN
0253-2964
Appears in Collections:
KIST Publication > Article
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