Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
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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
Drug Target Property Measurement pH Temperature (°C) Vildagliptin Dipeptidyl peptidase 4 IC 50 (nM) 51 8 37 Details