Acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) is of interest as a target for therapeutic treatment of diabetes, obesity and other diseases which together constitute the metabolic syndrome. In this poster we report our discovery and optimisation of a novel series of MGAT2 inhibitors. The development of the SAR of the series in lead generation phase as well as the development of the different chemistry routes will be disscussed. The in vivo results from an oral lipid tolerance test (OLTT) using the MGAT2 inhibitor (S)-10 , shows a significant reduction (68% inhibition relative to na?ve, p<0.01) in plasma triacylglycerol (TAG) concentration .

Identification and design of a novel series of MGAT2 inhibitors

246th National Meeting (2013)

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