کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1368971 981737 2015 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups
چکیده انگلیسی

Inhibitors of ghrelin O-acyltransferase (GOAT) have untapped potential as therapeutics targeting obesity and diabetes. We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ester bond in ghrelin and amide bonds in previously reported GOAT inhibitors. These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a foundation for rapid future chemical diversification and optimization of hGOAT inhibitors.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 14, 15 July 2015, Pages 2800–2803
نویسندگان
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