کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10591974 981769 2013 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification and design of a novel series of MGAT2 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification and design of a novel series of MGAT2 inhibitors
چکیده انگلیسی
[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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 9, 1 May 2013, Pages 2721-2726
نویسندگان
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