Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
J Med Chem
; 48(6): 1768-80, 2005 Mar 24.
Article
em En
| MEDLINE
| ID: mdl-15771423
ABSTRACT
The feasibility of the fluoro-olefin function as a peptidomimetic group in inhibitors for dipeptidyl peptidase IV and II (DPP IV and DPP II) is investigated by evaluation of N-substituted Gly-Psi[CF=C]pyrrolidines, Gly-Psi[CF=C]piperidines, and Gly-Psi[CF=C](2-cyano)pyrrolidines. Of this later class, the (Z)- and (E)-fluoro-olefin analogues were prepared and chemical stability in comparison with the parent amide was checked. Most of these compounds exhibited a strong binding preference toward DPP II with IC(50) values in the low micromolar range, while only low DPP IV inhibitory potential is seen.
Buscar no Google
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Inibidores de Proteases
/
Dipeptidil Peptidase 4
/
Dipeptidil Peptidases e Tripeptidil Peptidases
/
Alcenos
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article