Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.
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Wang L, Zhang B, Ji J, Li B, Yan J, Zhang W, Wu Y, Wang X
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.
Eur J Med Chem. 2009 Aug;44(8):3318-22. doi: 10.1016/j.ejmech.2009.03.021. Epub 2009 Mar 26.
- PubMed ID
- 19375196 [ View in PubMed]
- Abstract
To find potent and selective inhibitors of dipeptidyl peptidase IV (DPP-IV), we synthesized a series of 2-cyanopyrrolidine derivatives with constrained imidazolidin ring and tested their activities against DPP-IV. Most of them exhibited submicromolar inhibitory activities against DPP-IV. The most potent compound among these is (S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethyl-amino)acetyl)py rrolidine-2-carbonitrile (6n), which is a 2 nM DPP-IV inhibitor.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Saxagliptin Dipeptidyl peptidase 4 Ki (nM) 0.6 N/A N/A Details Sitagliptin Dipeptidyl peptidase 4 IC 50 (nM) 18 N/A N/A Details Vildagliptin Dipeptidyl peptidase 4 IC 50 (nM) 3.5 N/A N/A Details Vildagliptin Dipeptidyl peptidase 4 IC 50 (nM) 16.6 N/A N/A Details