Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

Article Details

Citation

Tsai TY, Coumar MS, Hsu T, Hsieh HP, Chien CH, Chen CT, Chang CN, Lo YK, Wu SH, Huang CY, Huang YW, Wang MH, Wu HY, Lee HJ, Chen X, Chao YS, Jiaang WT

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3268-72. Epub 2006 Apr 11.

PubMed ID
16581245 [ View in PubMed
]
Abstract

A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VildagliptinDipeptidyl peptidase 4IC 50 (nM)51837Details