Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Bioorg Med Chem Lett
; 15(19): 4239-42, 2005 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-16085416
ABSTRACT
The structure-activity relationship of various N-alkyl Gly-boro-Pro derivatives against three dipeptidyl peptidases (DPPs) was studied. In a series of N-cycloalkyl analogs, DPP4 and fibroblast activation protein-alpha (FAP) optimally preferred N-cycloheptyl whereas DPP7 tolerated even larger cycloalkyl rings. Gly alpha-carbon derivatization of N-cyclohexyl or N-(2-adamantyl) Gly-boro-Pro resulted in a significant decrease in potency against all the three DPPs.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Dipeptídeos
/
Dipeptidil Peptidases e Tripeptidil Peptidases
Limite:
Humans
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article