کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1357805 981283 2015 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and structure–activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes
ترجمه فارسی عنوان
طراحی، سنتز و ساختار فعالیت تحقیقاتی مرتبط با رونویسی فنوتیسیتی آمید آزاد مبتنی بر گیرنده 1 چربی آزاد برای درمان دیابت نوع 2
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Figure optionsDownload as PowerPoint slideThe free fatty acid receptor 1 (FFA1) has attracted extensive attention as a novel antidiabetic target in the last decade. Several FFA1 agonists reported in the literature have been suffered from relatively high molecular weight and lipophilicity. We have previously reported the FFA1 agonist 1. Based on the common amide structural characteristic of SAR1 and NIH screened compound, we here describe the continued structure–activity exploration to decrease the molecular weight and lipophilicity of the compound 1 series by converting various amide linkers. All of these efforts lead to the discovery of the preferable lead compound 18, a compound with considerable agonistic activity, high LE and LLE values, lower lipophilicity than previously reported agonists, and appreciable efficacy on glucose tolerance in both normal and type 2 diabetic mice.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 20, 15 October 2015, Pages 6666–6672
نویسندگان
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