کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1363694 | 981520 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A novel class of N-substituted 4-hydrazino piperidine derivatives were designed, synthesized and evaluated for DPP IV inhibition. The SAR studies on the N-substituted piperidine led to the discovery of compound 22e as a potent DPP IV inhibitor (IC50 88 nM), which is highly selective over other peptidases. In vivo efficacy indicates that compound 22e stimulates insulin release in response to glucose load and improves glucose tolerance in n5-STZ and Zucker Diabetic Fatty (ZDF) rats.
Various N-substituted (4-hydrazino piperidine) derivatives were synthesized and screened for in vitro DPP IV inhibition. In vivo efficacy of compound 22e has also been carried out.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5021–5025
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5021–5025
نویسندگان
Ramesh C. Gupta, Laxmikant Chhipa, Appaji B. Mandhare, Shitalkumar P. Zambad, Vijay Chauthaiwale, Sunil S. Nadkarni, Chaitanya Dutt,