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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of structurally novel, potent and orally efficacious GPR119 agonists
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.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 10, 15 May 2014, Pages 2383–2387
نویسندگان
, , , , , , , , , , , , , , , ,