کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377416 | 981977 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, calcium channel, Cyp2D6, and pharmacokinetic profiles.
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, L-type calcium channel, Cyp2D6, and pharmacokinetic profiles.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 16, 15 August 2007, Pages 4579–4583
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 16, 15 August 2007, Pages 4579–4583
نویسندگان
Jason M. Cox, Bart Harper, Anthony Mastracchio, Barbara Leiting, Ranabir Sinha Roy, Reshma A. Patel, Joseph K. Wu, Kathryn A. Lyons, Huaibing He, Shiyao Xu, Bing Zhu, Nancy A. Thornberry, Ann E. Weber, Scott D. Edmondson,