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Identification and design of a novel series of MGAT2 inhibitors
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2013 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1464-3405, Vol. 23, no 9, 2721-2726 p.Article in journal (Refereed) Published
Abstract [en]

[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 naive, p < 0.01) in plasma triacylglycerol (TAG) concentration.

Place, publisher, year, edition, pages
2013. Vol. 23, no 9, 2721-2726 p.
Keyword [en]
Monoacylglycerol acyltransferase, MGAT, Metabolic syndrome, Oral lipid tolerance test, Dioxotetrahydrobenzodiazepine
National Category
Medicinal Chemistry Organic Chemistry
URN: urn:nbn:se:su:diva-89981DOI: 10.1016/j.bmcl.2013.02.084ISI: 000317333900049OAI: diva2:622343


Available from: 2013-05-21 Created: 2013-05-20 Last updated: 2013-05-21Bibliographically approved

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Ertan, Anne
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Department of Materials and Environmental Chemistry (MMK)
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