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

摘要

We identified azabicyclo[3.1.0]hexane derivatives that are active diacylglycerol acyltransferasea??1 (DGAT)a??1 inhibitor. Among the azabicyclo[3.1.0]hexane series, compound 6b showed good in vitro activity toward human DGATa??1, selectivity toward DGATa??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.