کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369062 | 981744 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of structurally novel, potent and orally efficacious GPR119 agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Screening hit 5 was identified in a biochemical screen for GPR119 agonists. Compound 5 was structurally novel, displayed modest biochemical activity and no oral exposure, but was structurally distinct from typical GPR119 agonist scaffolds. Systematic optimization led to compound 36 with significantly improved in vitro activity and oral exposure, to elevate GLP1 acutely in an in vivo mouse model at a dose of 10 mg/kg.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 10, 15 May 2014, Pages 2383–2387
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 10, 15 May 2014, Pages 2383–2387
نویسندگان
Phil Alper, Mihai Azimioara, Christopher Cow, Daniel Mutnick, Victor Nikulin, Pierre-Yves Michellys, Zhiliang Wang, Esther Reding, Michael Paliotti, Jing Li, Dingjiu Bao, Jocelyn Zoll, Young Kim, Matthew Zimmerman, Todd Groessel, Tove Tuntland,