کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375231 | 981934 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of potent, orally active benzimidazole glucagon receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of potent, orally active benzimidazole glucagon receptor antagonists Discovery of potent, orally active benzimidazole glucagon receptor antagonists](/preview/png/1375231.png)
چکیده انگلیسی
The discovery and optimization of potent and selective aminobenzimidazole glucagon receptor antagonists are described. One compound possessing moderate pharmacokinetic properties in multiple preclinical species was orally efficacious at inhibiting glucagon-mediated glucose excursion in transgenic mice expressing the human glucagon receptor, and in rhesus monkeys. The compound also significantly lowered glucose levels in a murine model of diabetes.
Potent and selective aminobenzimidazole glucagon receptor antagonists are described. Compound 36 was orally efficacious in blocking glucagon-dependent glucose production and in lowering glucose levels in an animal model of diabetes.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 13, 1 July 2008, Pages 3701–3705
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 13, 1 July 2008, Pages 3701–3705
نویسندگان
Ronald M. Kim, Jiang Chang, Ashley R. Lins, Ed Brady, Mari R. Candelore, Qing Dallas-Yang, Victor Ding, Jasminka Dragovic, Susan Iliff, Guoqiang Jiang, Steven Mock, Sajjad Qureshi, Richard Saperstein, Deborah Szalkowski, Constantin Tamvakopoulos,