Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371431 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A series of novel [1,2,3]-triazolopiperidine derivatives 5a–5y were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes, most of the compounds exhibited excellent in vitro potency (IC50 <50 nM) against DPP-4. Among these, compound 5d with potent in vitro activity against DPP-4 and good pharmacokinetic profiles exhibited pronounced in vivo efficacy in an oral glucose tolerance test (OGTT) in ICR mice. On the base of these properties, compound 5d was selected as a potential new candidate for the treatment of type 2 diabetes.
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Related Topics
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Authors
Zhenwei Shan, Min Peng, Houxing Fan, Qingtao Lu, Peng Lu, Chuansheng Zhao, Yilang Chen,