Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1365200 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.
Graphical abstractThe synthesis, selectivity, rat pharmacokinetic profiles, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide