Triazolo compounds useful as diacylglycerol acyltransferase1 inhibitor – WO2009126624

Abstract

The accumulation of triacylglycerol in adipocytes causes obesity. Diacylglycerol acyltransferase (DGAT) catalyzes the final reaction of triacylglycerol synthesis. Two isozymes, DGAT1 and DGAT2, have been reported, and DGAT1 is considered a potential therapeutic target of inhibition for obesity control. Patent WO2009126624 proposes 69 new triazolopyridine compounds as DGAT1 inhibitors by Bristol-Myers Squibb. The inhibitory activity of these triazolopyridine compounds was assessed in an enzyme assay using microsomal fractions prepared from human DGAT1-expressing insect cells. Among them, four derivatives inhibited DGAT activity with IC₅₀ values of < 0.1 μM.

Keywords::

• DGAT
• obesity
• triacylglycerol
• triazolopyridine