Triazolo compounds useful as diacylglycerol acyltransferase1 inhibitor - WO2009126624.
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 IC(50) values of < 0.1 microM.
Kitasato University, Minato-ku, Tokyo, Japan.
Daisuke
D
Matsuda
Hiroshi
H
Tomoda
D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000494:pharmacology*; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D014280:Triglycerides / Q000096:biosynthesis
D019440:Anti-Obesity Agents; D004791:Enzyme Inhibitors; D014230:Triazoles; D014280:Triglycerides; C494881:DGAT1 protein, human; D051048:Diacylglycerol O-Acyltransferase