کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372812 981882 2008 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
چکیده انگلیسی

Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed excess plasma glucose to ameliorate diabetes-related hyperglycemia and associated complications. The current study demonstrates that the proper relationship of a 4′-substituted benzyl group to a β-1C-phenylglucoside is important for potent and selective SGLT2 inhibition. The lead C-arylglucoside (7a) demonstrates superior metabolic stability to its O-arylglucoside counterpart (4) and it promotes glucosuria when administered in vivo.

The evolution of potent and selective C-arylglucoside SGLT2 inhibitors from lead 6 to 7a is described.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 17, 1 September 2008, Pages 4770–4773
نویسندگان
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