کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374462 | 981919 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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![عکس صفحه اول مقاله: Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy](/preview/png/1374462.png)
چکیده انگلیسی
Key binding interactions of the anthranilimide based glycogen phosphorylase a (GPa) inhibitor 2 from X-ray crystallography studies are described. This series of compounds bind to the AMP site of GP. Using the binding information the core and the phenyl urea moieties were optimized. This work culminated in the identification of compounds with single nanomolar potency as well as in vivo efficacy in a diabetic model.
Use of an X-ray crystal structure allowed for the optimization of the anthranilimide-based glycogen phosphorylase inhibitors to give compound 23 which displayed both in vitro potency versus GPa and in vivo efficacy in a mouse model of type 2 diabetes.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 4, 15 February 2009, Pages 1177–1182
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 4, 15 February 2009, Pages 1177–1182
نویسندگان
Stephen A. Thomson, Pierette Banker, D. Mark Bickett, Joyce A. Boucheron, H. Luke Carter, Daphne C. Clancy, Joel P. Cooper, Scott H. Dickerson, Dulce M. Garrido, Robert T. Nolte, Andrew J. Peat, Lauren R. Sheckler, Steven M. Sparks, Francis X. Tavares,