Discovery of potent dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes.

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Shan Z, Peng M, Fan H, Lu Q, Lu P, Zhao C, Chen Y

Discovery of potent dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1731-5. doi: 10.1016/j.bmcl.2011.01.086. Epub 2011 Jan 22.

PubMed ID
21334204 [ View in PubMed
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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 (IC(50)<50n M) 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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SitagliptinDipeptidyl peptidase 4IC 50 (nM)19.4N/AN/ADetails