کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376556 | 981961 | 2008 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1–8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds synthesized showed significant lowering of plasma glucose level in this model. As a possible mode of action, the compounds were in vitro evaluated as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. The most active compounds (3 and 4) were docked into the crystal structure of 11β-HSD1. Docking results indicate potential hydrogen bond interactions with catalytic amino acid residues.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 9, 1 May 2008, Pages 2871–2877
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 9, 1 May 2008, Pages 2871–2877
نویسندگان
Hermenegilda Moreno-Díaz, Rafael Villalobos-Molina, Rolffy Ortiz-Andrade, Daniel Díaz-Coutiño, Jose Luis Medina-Franco, Scott P. Webster, Margaret Binnie, Samuel Estrada-Soto, Maximiliano Ibarra-Barajas, Ismael León-Rivera, Gabriel Navarrete-Vázquez,