A series of (4-substituted prolyl)prolinenitriles were synthesized and evaluated as inhibitors of dipeptidylpeptidase IV (DPP-IV). Among those tested, the 4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles showed a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates was found to contribute to their long duration of action. The activity profiles of the synthesized compounds are reported and structure-activity relationships are also presented.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2007.01.033 | DOI Listing |
Publication Analysis
Top Keywords
long duration
8
duration action
8
design synthesis
4
synthesis long-acting
4
long-acting inhibitors
4
inhibitors dipeptidyl
4
dipeptidyl peptidase
4
peptidase series
4
series 4-substituted
4
4-substituted prolylprolinenitriles
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!