The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.
Bioorg Med Chem Lett
; 26(11): 2622-6, 2016 06 01.
Article
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| MEDLINE
| ID: mdl-27106708
ABSTRACT
Novel potent and selective 5,6,5- and 5,5,6-tricyclic pyrrolidine dipeptidyl peptidase IV (DPP-4) inhibitors were identified. Structure-activity relationship (SAR) efforts focused on improving the intrinsic DPP-4 inhibition potency, increasing protease selectivity, and demonstrating clean ion channel and cytochrome P450 profiles while trying to achieve a pharmacokinetic profile suitable for once weekly dosing in humans.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirrolidinas
/
Dipeptidil Peptidasa 4
/
Inhibidores de la Dipeptidil-Peptidasa IV
/
Descubrimiento de Drogas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2016
Tipo del documento:
Article