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Synthesis and Diacylglycerol Acyltransferase-1 Inhibition of Azabicyclo[3.1.0]hexane Derivatives
한서정,이귀빈,곽현정,Suvarna H. Pagire,김지영,Haushabhau S. Pagire,박성범,채정학,이주윤,김기영,이상달,김희연,신선혜,배명애,박미진,김두섭,이덕형,안진희 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.6
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.