Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.

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Cho TP, Long YF, Gang LZ, Yang W, Jun LH, Yuan SG, Hong FJ, Lin W, Liang GD, Lei Z, Jing LJ, Shen GA, Hong SG, Dan W, Ying F, Ke YP, Ying L, Jun F, Tai MX

Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3565-8. doi: 10.1016/j.bmcl.2010.04.120. Epub 2010 May 18.

PubMed ID
20488702 [ View in PubMed
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Abstract

A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VildagliptinDipeptidyl peptidase 4IC 50 (nM)9N/AN/ADetails