کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365539 | 981564 | 2007 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.
Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as dipeptidyl peptidase IV (DPP-4) inhibitors. The in vitro profile of these compounds is described, and in vivo efficacy and pharmacokinetics are also presented.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 21, 1 November 2007, Pages 5934–5939
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 21, 1 November 2007, Pages 5934–5939
نویسندگان
Jennifer E. Kowalchick, Barbara Leiting, KellyAnn D. Pryor, Frank Marsilio, Joseph K. Wu, Huaibing He, Kathryn A. Lyons, George J. Eiermann, Aleksandr Petrov, Giovanna Scapin, Reshma A. Patel, Nancy A. Thornberry, Ann E. Weber, Dooseop Kim,