Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.
J Med Chem
; 50(23): 5568-70, 2007 Nov 15.
Article
em En
| MEDLINE
| ID: mdl-17958345
ABSTRACT
Dipeptide-derived compounds, bearing various P2 residues and a diaryl pyrrolidin-2-yl phosphonate at the P1 position, were evaluated as dipeptidyl peptidase 8 (DPP8) inhibitors. With these products, irreversible inhibition of DPP8 was observed. To obtain inhibitors with an improved activity and selectivity profile, a set of selected analogues containing a diaryl isoindolin-1-ylphosphonate at P1 was synthesized and evaluated. Within this latter series, compound 2e was shown to be a potent, irreversible inhibitor of DPP8, demonstrating very low affinity for DPP IV and DPP II.
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Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Dipeptidases
/
Dipeptídeos
/
Isoindóis
/
Organofosfonatos
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
Bélgica