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Bioorg Med Chem Lett. 2013 May 1;23(9):2721-6. doi: 10.1016/j.bmcl.2013.02.084. Epub 2013 Feb 27.

Identification and design of a novel series of MGAT2 inhibitors.

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AstraZeneca R&D, Cardiovascular & Gastrointestinal Innovative Medicines Unit Mölndal, SE-431 83 Mölndal, Sweden.


[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 Letter we report our discovery and optimisation of a novel series of MGAT2 inhibitors. The development of the SAR of the series and a detailed discussion around some key parameters monitored and addressed during the lead generation phase will be given. 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 naїve, p<0.01) in plasma triacylglycerol (TAG) concentration.

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