کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371818 | 981856 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. Compound 16 (APD597, JNJ-38431055) was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug–drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long lasting metabolites with the potential to accumulate in clinical studies.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1750–1755
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1750–1755
نویسندگان
Graeme Semple, Juerg Lehmann, Amy Wong, Albert Ren, Marc Bruce, Young-Jun Shin, Carleton R. Sage, Michael Morgan, Wei-Chao Chen, Kristen Sebring, Zhi-Liang Chu, James N. Leonard, Hussein Al-Shamma, Andrew J. Grottick, Fuyong Du, Yin Liang,