Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591974 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
[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 naÑve, p <0.01) in plasma triacylglycerol (TAG) concentration.
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Authors
Jonas G. Barlind, Linda K. Buckett, Sharon G. Crosby, Ãjvind Davidsson, Hans Emtenäs, Anne Ertan, Ulrik Jurva, Malin Lemurell, Pablo Morentin Gutierrez, Karolina Nilsson, Gavin O'Mahony, Annika U. Petersson, Alma Redzic, Fredrik WÃ¥gberg,